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Sample search results for: a1 receptor antagonist

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1 Nonpeptide antagonists of neuropeptide receptors: Tools for research and therapy
 

Summary:  Nonpeptide antagonists of neuropeptide receptors: Tools for research and therapy Catalina Betancur... @adr.st-antoine.inserm.fr Running title: Nonpeptide antagonists of peptide receptors Key words: nonpeptide antagonist, peptide... the discovery of the first nonpeptide ...

  

Source: Ecole Polytechnique, Centre de mathématiques

 

Collection: Mathematics

 
2 Stimulating electrode AMPA receptor
 

Summary:  GABAB receptor Agonist = baclofen Antagonist = phaclofen Antagonist = 2-amino-5-phosphonovaleric acid... (AP5 or APV) Antagonist = 6-cyano-7-nitro-quinoxaline- (CNQX) mGluR mGluR receptor: Agonist = 2-amino... 2,3-dione Glutamate Glu GABA NMDA AMPA Na+ Na+ & Ca++ K+ Stimulating ...

  

Source: Hasselmo, Michael - Department of Psychology & Computational Neurophysiology Laboratory, Boston University

 

Collection: Biology and Medicine

 
3 This article was originally published in the Encyclopedia of Neuroscience published by Elsevier, and the attached copy is provided by Elsevier for the
 

Summary:  antagonists. DPCPX (8-cyclopentyl-1,3- dipropylxanthine) is an A1 receptor antagonist with subnanomolar... Four different P1 receptor subtypes, A1, A2A, A2B, and A3, have been cloned. All are G... transmembrane domain (see ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
4 Dual constrictor and dilator actions of ETB receptors in the rat renal microcirculation: interactions with ETA receptors
 

Summary:  receptors is based mainly on effects of ETA-specific antagonists. The contribution of ETB... the injection. To achieve ET receptor inhibition, saline was replaced by an infusion of an antagonist (7 nmol... using the same protocol, except that the ETB-receptor ...

  

Source: Just, Armin - Physiologisches Institut I, Albert-Ludwigs-Universität Freiburg

 

Collection: Biology and Medicine

 
5 oo26-895x196/o3o54o-o7$3.oo/o Copyright by The American Society for Pharmacology and Experimental Therapeutics
 

Summary:  with a Kb of 6 p.M while inhibiting AMPA receptors with a Kb of >100 p.M. The remaining antagonists showed... competitive antagonists block native AMPA and kainate receptors with approximately similar potencies, which... receptor subtypes is based largely on studies involving ...

  

Source: Huettner, James E. - Department of Cell Biology and Physiology, Washington University in St. Louis

 

Collection: Biology and Medicine

 
6 Introduction Chapter 1 1 Introduction
 

Summary:  ; however, the receptors were not susceptible to blockade by selective 5-HT2 and 5-HT3 antagonists19... receptor selective antagonist, revealed that this receptor subtype is not likely to act as an autoreceptor... receptor antagonist was unable to ...

  

Source: Groningen, Rijksuniversiteit - Centre for Ecological and Evolutionary Studies, Department of Marine Benthic Ecology and Evolution,

 

Collection: Biology and Medicine ; Environmental Sciences and Ecology

 
7 J Neural Transm (2007) 114: 4975 DOI 10.1007/s00702-006-0589-0
 

Summary:  receptor (see Marshall, 2005). Also the A1R= P2Y1R heteromerization leads to the appearance of an A1... accumbens (Diaz-Cabiale et al., 2001). In higher doses CGS 21680 but not an A1 receptor agonist could antag... for ...

  

Source: Chin-Sang, Ian - Department of Biology, Queen's University (Kingston)

 

Collection: Biology and Medicine

 
8 Diinosine pentaphosphate: an antagonist which discriminates between recombinant P2X3 and P2X2/3 receptors and between two
 

Summary:  with an IC50 of 0.1 mM. Both antagonists are known to inhibit homomeric P2X3 receptors. 5 Some DRG neurones... In conclusion, Ip5I is a potent antagonist at homomeric P2X3 receptors but not at heteromeric P2X2/3 receptors... and antagonists will help to clarify the ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
9 2001 Wiley-Liss, Inc. DRUG DEVELOPMENT RESEARCH 53:281291 (2001)
 

Summary:  -4), histamine (H1), serotonin (5-HT3) or adenosine (A1 and A2B) receptors [Lambrecht et al., 1992, 2000; Boyer... can be altered at the pyridoxal and phenyl moieties to produce P2X1 and P2X3 receptor antagonists... ,5 -monophosphate (MRS 2219, a cyclized form of P5P) lost ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
10 Hypocretins (1 and 2, aka. Orexin A and B) are neuropeptides synthesized in the lateral hypothalamus and are important contributors to arousal state, thermoregulation and
 

Summary:  slice preparations only, and hypocretin receptor antagonists have more severe effects in WT... /f/p slices do not response to acidosis (pH 6.9). · Hypocretin receptor antagonists do not inhibit... in situ Figure 5. Effect of SB-408124 (hypocretin 1 receptor, hcrt-r1, ...

  

Source: Wagner, Diane - Institute of Arctic Biology, Department of Biology and Wildlife, University of Alaska Fairbanks

 

Collection: Environmental Sciences and Ecology

 
11 Constitutive Activity of a Chimeric D2/D1 Dopamine Receptor LAURA B. KOZELL and KIM A. NEVE
 

Summary:  also inverse agonists at the D1 receptor. Interestingly, several antagonists also potentiated forskolin... ) where TABLE 1 Affinity of D1, D2, and chimeric dopamine receptors for antagonists Ki values... expressing D1 receptors. The D1-selective antagonist, SCH23390, ...

  

Source: Neve, Kim A. - Department of Behavioral Neuroscience, Oregon Health and Science University

 

Collection: Biology and Medicine

 
12 Bruce N. Cronstein, MD You Are Not Arthur Conan Doyle
 

Summary:  Data "Adenosine A1 receptor activation stimulates SREBP1 translocation... by either an adenosine A1 or A2B antagonist and mice deficient in these adenosine... problem. Moreover, the demonstration that ...

  

Source: Wang, Da-Neng - Skirball Institute of Biomolecular Medicine & Department of Cell Biology, New York University

 

Collection: Biology and Medicine

 
13 Allosteric Modulation of 2-Adrenergic Receptor by Zn2 GAYATHRI SWAMINATH, JACQUELINE STEENHUIS, BRIAN KOBILKA, and TAE WEON LEE
 

Summary:  , allosteric com- pounds have been identified for the A1 adenosine receptor. The 2-amino-3-benzoylthiophene PD... ) The allosteric enhancer, PD 81,723, stabilizes human A1 adenosine receptor coupling to G proteins. Biochim... 258:3913­3919. Musser B, Mudumbi RV, Liu ...

  

Source: Kobilka, Brian - Department of Molecular and Cellular Physiology, Stanford University

 

Collection: Biology and Medicine

 
14 Corticotropin-Releasing Factor-1 Receptor Activation Mediates Nicotine Withdrawal-Induced Deficit in Brain
 

Summary:  that blockade of corticotropin-releasing factor (CRF) receptors with a nonspecific CRF1/CRF2 receptor antagonist... , the nicotinic receptor antagonist mecamylamine elevated the brain reward thresholds of the nicotine- dependent... rats but not those of the control rats. The CRF1 ...

  

Source: Príncipe, José Carlos - Computational NeuroEngineering Laboratory, University of Florida

 

Collection: Engineering ; Computer Technologies and Information Sciences

 
15 The concept of purinergic neurotransmission was pro-posed in 1972 (REF. 1), after it was shown that adenosine
 

Summary:  inhibitory modulator through P1(A1 ) receptors, but ATP itself can act presynaptically either to inhibit... , and in a rat model of Parkinson's disease, A1 , dopamine D1 and glutamate mGlu5 receptors have been shown... presynaptic ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
16 ELSEVIER Brain Research 672 (1995) 42-47 Research report
 

Summary:  that chronic opioid antagonists, acting on K and p~ opioid receptors, clearly up-regulate prodynorphin gene... of receptors available [7,19,29,31,35]. However, chronic treatment with opiate antagonists reportedly increases... [22-25]. Nor-binaltorphimine (nor-BNI) [28], a highly selec- tive ...

  

Source: Lesa, Giovanni - Department of Physiology, University College London

 

Collection: Biology and Medicine

 
17 Biochem. J. (2001) 354, 485491 (Printed in Great Britain) 485 Tyr199 in transmembrane domain 5 of the 2-adrenergic receptor interacts
 

Summary:  been reported. To identify receptor amino acids that contribute to the # AR antagonist binding site... +-nitrilotriacetate; Endo Lys-C, endoproteinase Lys-C; Con A, concanavalin A. 1 Present address: Du... of physical interaction between a # AR antagonist and the ...

  

Source: Kalil, Ronald E. - Neuroscience Training Program & W.M. Keck Laboratory for Biological Imaging, University of Wisconsin at Madison

 

Collection: Biology and Medicine

 
18 Diabetes Metab . Author manuscript Cannabinoid receptors as novel therapeutic targets for the management of
 

Summary:  in several countries for the management of chemotherapy-induced nausea and vomiting ( ) and rimonabant, a1... selective CB1 receptor antagonist has been available since 2 years in Europe as an adjunctive treatment... agonists and antagonists of CB2 receptors have not ...

  

Source: Ecole Polytechnique, Centre de mathématiques

 

Collection: Mathematics

 
19 ABSTRACT The concept of a purinergic sig-nalling system, using purine nucleotides and
 

Summary:  were due to indirect action via P1 receptors. Four subtypes of P2 receptors were cloned, namely A1, A2A... . The antithrombotic action of clopidogrel (Plavix), a P2Y12 receptor antagonist, has been shown to be particularly... antagonist. Since ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
20 The structure of active opsin as a basis for identification of GPCR agonists by dynamic homology modelling and virtual screening assays
 

Summary:  modelling and virtual screening assays Michael Schneider a,1 , Steffen Wolf a,b , Jürgen Schlitter a , Klaus... an inactive receptor state, which has been considered to be suitable only for the discovery of antagonists... t Most of the currently available G protein-coupled receptor ...

  

Source: Gerwert, Klaus - Fakultät für Biologie, Ruhr-Universität Bochum

 

Collection: Biology and Medicine


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21 P2 receptor web: Complexity and fine-tuning Cinzia Volont a,, Susanna Amadio a
 

Summary:  , zinc and copper and generic P2X receptor antagonists. Nevertheless, currents are relatively insensitive... ., 2002; Jacobson et al., 2004), a selective antagonist at P2 receptor versus other types of receptors... , but not a universal P2 receptor ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
22 ABBREVIATIONS: NMDA, N-methyl-D-aspartate; AMPA, ct-amino-3-hydroxy-4-methylisoxazolepropionic acid; DDB, 2,5-dihydro-2,5-dioxo-1H-ben-zazepine; DDHB, 2,5-dihydro-2,5-dioxo-3-hydroxy-1H-benzazepine; 4-Br-DDHB, 7-Me-DDHB, and 8-Me-DDHB, 4-bromo, 7-methyl,
 

Summary:  M DDHB Fig. 1. Parent structures of glutamate receptor antagonists. iJ_l-J-----l\_ ---. NMDA 20 p... ) (1 3 applications in four cells) or in the presence of 8 8-Me-DDHB (A) (1 3 applications in five... ). These compounds represent a new class of competitive gluta- mate receptor ...

  

Source: Huettner, James E. - Department of Cell Biology and Physiology, Washington University in St. Louis

 

Collection: Biology and Medicine

 
23 Perspectives in Pharmacology P2 Purinergic Receptors: Modulation of Cell Function and
 

Summary:  this response. AMP gives rise to adenosine, which acti- vates the various P1 receptors (A1, A2A, A2B, A3... of available P2 receptor antagonists are relatively weak and only mar- ginally selective for one P2 receptor... and Knutsen, 2001). Putative P2 ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
24 Structure-Activity Relationships of Pyridoxal Phosphate Derivatives as Potent and Selective Antagonists of P2X1 Receptors
 

Summary:  Antagonists of P2X1 Receptors Yong-Chul Kim, Sean G. Brown, T. Kendall Harden,§ Jose´ L. Boyer,§ George Dubyak... of the P2 receptor antagonist pyridoxal-5-phosphate 6-azophenyl-2,5- disulfonate (2) were synthesized... and studied as antagonists in functional assays at recombinant rat ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
25 Vol. 275, No. 3 Printed in U.S.A.
 

Summary:  Glutamate Receptor Antagonist R. M. WOODWARD, J. E. HUETTNER1, M. IRAN, J. GUASTELLA, J. F. W. KEANA2 and E... is a competitive antagonist at NMDA receptor glycine sites. Apparent antagonist affinities (Kb values) were 0... - tropic glutamate receptor ...

  

Source: Huettner, James E. - Department of Cell Biology and Physiology, Washington University in St. Louis

 

Collection: Biology and Medicine

 
26 Pharmacological characterization of serotonin receptor subtypes modulating primary aerent input to deep dorsal horn neurons in
 

Summary:  University, Atlanta, Georgia, GA 30322, U.S.A. 1 Spinal cord slices and whole-cell patch clamp recordings... 7 receptor antagonist clozapine and was not observed in the presence of NAN-190, a 5-HT1A receptor... antagonist. In the absence of any agonist, 5-HT1A ...

  

Source: Hochman, Shawn - Department of Physiology, Emory University

 

Collection: Biology and Medicine

 
27 Enhancement of the surface expression of G protein-coupled receptors
 

Summary:  -terminus of the a1D-adrenoceptor (a1D-AR) dramatically enhanced expression of receptor binding sites [25] and plasma... impaired surface expression of these receptors in heterologous cells [26], suggesting that the a1D-AR N... ...

  

Source: Hall, Randy A - Department of Pharmacology, Emory University

 

Collection: Biology and Medicine

 
28 Progress in Neurobiology 70 (2003) 387407 Kainate receptors and synaptic transmission
 

Summary:  M CGP55845) or adenosine A1 (0.1 M DPCPX) receptors. Similar results were obtained by Kamiya... - sure to the GABAB receptor agonist baclofen (10 M), the A1 adenosine receptor agonist 2-chloroadenosine... , GABAB, muscarinic or adenosine ...

  

Source: Huettner, James E. - Department of Cell Biology and Physiology, Washington University in St. Louis

 

Collection: Biology and Medicine

 
29 Purinergic signalling: therapeutic potential* GEOFFREY BURNSTOCK
 

Summary:  receptors were cloned, namely A1, A2A, A2B and A3 and in 1985, Burnstock and Kennedy proposed a basis... receptor antagonist, has been shown to be particularly useful in the prevention of recurrent strokes... , which are antagonists to the platelet P2Y12 ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
30 Reduction of Stress-Induced Behavior by Antagonism of Corticotropin-Releasing Hormone 2 (CRH2) Receptors in Lateral
 

Summary:  ]sauvagine binding in the LS could be inhibited by a CRH1 /CRH2 antagonist but not by the selective CRH1 receptor... antagonist, confirming that in the LS, hCRH antagonized exclusively CRH2 receptors. Acute antag- onism of CRH... behaviors normally exhibited in response to stress, whereas CRH ...

  

Source: Kalil, Ronald E. - Neuroscience Training Program & W.M. Keck Laboratory for Biological Imaging, University of Wisconsin at Madison

 

Collection: Biology and Medicine

 
31 Z .Brain Research 757 1997 276279 Short communication
 

Summary:  , these antagonists have a lower affinity for opioid receptors than their tertiary parent compounds. The relative... affinity of quaternary vs. tertiary antagonists either for opioid receptors in non-mammalian species... with opioid receptor antagonists such as Z . Z ...

  

Source: Deviche, Pierre - Department of Biology, Arizona State University

 

Collection: Biology and Medicine

 
32 Current Pharmaceutical Design, 2009, 15, 000-000 1 1381-6128/09 $55.00+.00 2009 Bentham Science Publishers Ltd.
 

Summary:  also form heterodimeric com- plexes [64] or with other receptors. For example, adenosine A1 receptors... and adenosine A1 receptors have also been shown to form func- tionally interactive heteromeric complexes. D. ATP... , although they have yet ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
33 Current Topics in Medicinal Chemistry 2004, 4, 793-803 793 1568-0266/04 $45.00+.00 2004 Bentham Science Publishers Ltd.
 

Summary:  of mammalian P2Y1 receptors [34], and MRS 2179 is a potent antagonist [35]; MRS 2269 and MRS 2286 have been... identified as selective antagonists [36]. At P2Y2 and P2Y4 receptors in the rat, ATP and UTP are equipotent... , but the two receptors can be distinguished with ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
34 NPY signaling through Y1 receptors modulates thalamic oscillations
 

Summary:  ). Effects of the Y1 receptor agonist Leu31Pro34NPY (A1 and A2), the Y2 receptor agonist PYY3­36 (B1 and B2... ) and the Y5 receptor agonist BWX-46 (C1 and C2). A1, B1 and C1: Contour plots representing ratemeter... capsule (A2, B2 and C2). ...

  

Source: Huguenard, John R. - Department of Neurology and Neurological Sciences, Stanford University

 

Collection: Biology and Medicine

 
35 PharmacologyBiochemistry&Behavior.Vol.22. pp. 341-342, 1985.AnkhoInternationallnc, Printedin the U,S.A. 0091-3057/85$3.00 + .00 BRIEF COMMUNICATION
 

Summary:  ,S.A. 0091-3057/85$3.00 + .00 BRIEF COMMUNICATION The D1 Dopamine Receptor Antagonist, SCH 23390 Reduces... and rearing. SCH 23390 DI receptor antagonist Locomotor activity and rearing AT least two different receptor... by the development of specific DA antagonists ...

  

Source: Beninger, Richard J. - Department of Psychology, Queen's University (Kingston)

 

Collection: Biology and Medicine

 
36 The recently deorphanized GPR80 (GPR99) proposed to be the P2Y15 receptor is not a genuine P2Y receptor
 

Summary:  the pharmacological characterization of novel receptors. Moreover, adenosine A1 and P2Y1 receptors have been shown... previously to form heterodimers that enable the A1 receptor to bind and respond to ADP [6], and thus... ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
37 D2/D3 Dopamine Receptor Heterodimers Exhibit Unique Functional Properties*
 

Summary:  for heterodimerization has recently been provided for dopamine D1 and adenosine A1 receptors as well as for dopamine D2... receptor forms hetero-oligomers with the adenosine A1 receptor. As the issue of G protein-coupled ...

  

Source: Vogel, Zvi - Department of Neurobiology, Weizmann Institute of Science

 

Collection: Biology and Medicine

 
38 International Union of Pharmacology LVIII: Update on the P2Y G Protein-Coupled Nucleotide Receptors
 

Summary:  of selective agonists and antagonists to some of the P2Y receptor subtypes. There are new findings about... International Union of Pharmacology LVIII: Update on the P2Y G Protein-Coupled Nucleotide Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
39 Purine and pyrimidine receptors G. Burnstock
 

Summary:  antagonists. DPCPX (8-cyclopentyl-1,3-dipropylxanthine) is an A1 receptor antagonist with sub... by ectonucleotidases. Four subtypes have been identified, A1, A2A, A2B and A3 receptors. P2 receptors are ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
40 Purine and pyrimidine receptors G. Burnstock
 

Summary:  antagonists. DPCPX (8-cyclopentyl-1,3-dipropylxanthine) is an A1 receptor antagonist with sub... , complementary DNAs (cDNAs) encoding two different P1 receptor subtypes (A1 and A2) were isolated [20], and... , shortly after, ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine


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41 Brain Research 902 (2001) 1117 www.elsevier.com/locate/bres
 

Summary:  , WT F2 progeny with two WT 129 5-HT1A 1A receptor antagonist, also enhances SSRI-evoked increases... -selective 5-HT receptor antagonist WAY 100,635 1A 1A physiological studies in the rat brain, Synapse 1 (1987... of central ...

  

Source: Sibille, Etienne - Center for the Neural Basis of Cognition & Department of Psychiatry, University of Pittsburgh

 

Collection: Biology and Medicine

 
42 nature neuroscience volume 4 no 4 april 2001 417 Glutamate is the predominant excitatory neurotransmitter in
 

Summary:  of NMDA receptors to DHPG-induced thermal hypersensitivity30, we injected APV, an NMDA receptor antagonist... - eral injection of excitatory amino acids have also found that NMDA or AMPA receptor antagonists... not reduce DHPG-induced thermal hyper- sensitivity. (a) Pretreatment with APV ...

  

Source: Steinbach, Joe Henry - Washington University Pain Center & Department of Anesthesiology, Washington University in St. Louis

 

Collection: Biology and Medicine

 
43 REVIEW ARTICLE Chemokine receptors and other G protein-coupled receptors
 

Summary:  D, Zhang L, et al. Heterologous expression of the adenosine A1 receptor in transgenic mouse retina... are antagonists to the CCR5 receptor, are in clinical use or in clinical trials [15]. These com- pounds can block... to antagonist-bound CCR5 ...

  

Source: Palczewski, Krzysztof - Department of Pharmacology, Case Western Reserve University

 

Collection: Biology and Medicine

 
44 Structure based prediction of subtype-selectivity for adenosine receptor antagonists
 

Summary:  into the structural basis of ligand subtype selectivity within the family of adenosine receptors (AR: A1, A2A, A2B... ) of ligand and decoy sets were similar. 2.2. Homology modeling of A1, A2B and A3 adenosine receptor subtypes... compounds lacking the exocyclic ...

  

Source: Abagyan, Ruben - School of Pharmacy and Pharmaceutical Sciences, University of California at San Diego

 

Collection: Biology and Medicine

 
45 Research Signpost 37/661 (2), Fort P.O., Trivandrum-695 023, Kerala, India
 

Summary:  by the selective A1 receptor antagonist 8- cyclopentyl-1,3-dipropylxanthine (DPCPX). The ecto-ATPase inhibitor (ARL... nervous system. P2X3 receptor antagonists are being explored for alleviating renal colic. ATP contracts... consisted of both fast and slow ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
46 NEUROKININ RELEASE IN THE RAT NUCLEUS OF THE SOLITARY TRACT VIA NMDA AND AMPA RECEPTORS
 

Summary:  in vitro brainstem slices, immunoreactivity for NK1 receptor (Fig. 2A, A1) and NK3 receptors (Fig. 3D... internalization in neurons of the NST. (A^A1) NK1 receptor immunoreactivity is located on the surface of neurons... by the endocytosis ...

  

Source: Cossart, Rosa - Institut de Neurobiologie de la Méditerranée, Inserm

 

Collection: Biology and Medicine

 
47 The role of central dopamine D3 receptors in drug addiction: a review of pharmacological evidence
 

Summary:  ]). BP-897 also displays potent antagonistic action at 5-HT2A and a1- adrenergic receptors (M.J. Millan... is referred to Ref. [103]). BP-897 shows moderate affinity for a1- and a2-adrenergic receptors (Ki = 60 and 83... . Currently, with the ...

  

Source: Brookhaven National Laboratory, Environmental Chemistry Division, Department of Applied Science

 

Collection: Environmental Sciences and Ecology

 
48 Heterodimerization of G Protein-Coupled Receptors: Specificity and Functional Significance
 

Summary:  GPCRs (A1, A2A, A2b, and A3), whereas ATP activates P2X receptors, which are ion channels, as well... heterodimerization between purinergic receptor subtypes has been reported for A1R and P2Y1R in both transfected cells... dopamine receptors ...

  

Source: Hall, Randy A - Department of Pharmacology, Emory University

 

Collection: Biology and Medicine

 
49 Muscarinic M3-receptors mediate cholinergic synergism of mitogenesis in
 

Summary:  significantly by the selective M3-receptor antagonists DAU5884 (0.1 µM) and 4-DAMP (10 nM), but not at all... measured the inhibitory effects of selective receptor antagonists (DAU5884, 4-DAMP and gallamine... (open circles) or presence of 0.1 µM (filled circles, panel A), ...

  

Source: Groningen, Rijksuniversiteit - Centre for Ecological and Evolutionary Studies, Department of Marine Benthic Ecology and Evolution,

 

Collection: Biology and Medicine ; Environmental Sciences and Ecology

 
50 *MRC Laboratory of Molecular Biology,
 

Summary:  receptors and was blocked by the antagonist PPADS (pyridoxal phosphate 6-azophenyl-2,4-disulphonic acid)5... of the non-NMDA glutamate receptor antagonist CNQX (6-cyano-7-nitroquinoxaline-2,3-dione)6 . Washout of CNQX... moiety of the ATP receptor antagonist N C The ...

  

Source: Lester, Henry - Division of Biology, California Institute of Technology

 

Collection: Biology and Medicine

 
51 0022.3565/87/2423-0882S00.00/0 THE JOURNALor PHARMACOLOGYAND EXP!JUNENTALTHERAPEIITICS
 

Summary:  adenosine receptors in this re- sponse. The potent antagonist XAC displayed considerable A1 selectivityas... potent, A1-selective adenosine receptor antagonist with high water solubility and subsequent... t'.S.A. ...

  

Source: Wurtman, Richard - Department of Brain and Cognitive Science, Massachusetts Institute of Technology (MIT)

 

Collection: Biology and Medicine

 
52 Rational discovery of novel nuclear hormone receptor antagonists
 

Summary:  Rational discovery of novel nuclear hormone receptor antagonists Matthieu Schapira* , Bruce M... , with the exception of the human estrogen receptor- , the lack of antagonist-bound ``inactive'' receptor structures... receptor- by using informa- tion derived from ...

  

Source: Abagyan, Ruben - School of Pharmacy and Pharmaceutical Sciences, University of California at San Diego

 

Collection: Biology and Medicine

 
53 Novel Treatment for Stroke, Brain Trauma, Alzheimer's Disease and
 

Summary:  cell death, unlike previous non-specific NMDA receptor antagonists Principal Inventor(s): Dr. Yu Tian... survival. This explains why previous non-specific NMDA receptor antagonists have failed in all clinical... while co-administering glycine (the co-agonist of NMDA receptors) and an ...

  

Source: Michelson, David G. - Department of Electrical and Computer Engineering, University of British Columbia

 

Collection: Engineering

 
54 The serotonergic system The Serotonergic System
 

Summary:  shown that 5-HT2A receptor increases cAMP in A1A1 adrenal cells by the intermediary action of calmodulin... animals were insensitive to the hyperlocomotor effects of the 5-HT1A/1B receptor agonist RU... are tryptamine ...

  

Source: Groningen, Rijksuniversiteit - Centre for Ecological and Evolutionary Studies, Department of Marine Benthic Ecology and Evolution,

 

Collection: Biology and Medicine ; Environmental Sciences and Ecology

 
55 Regulation of Neurotransmitter Release by Metabotropic Glutamate Receptors
 

Summary:  ), respectively. A brief overview of only the various agonists and antagonists of mGlu receptor subtypes that have... -dicarboxycyclopropyl)glycine (DCG-IV) has high potency at mGlu2/3 receptors, it also has antagonist actions at group... section). Of the five antagonists shown in Table ...

  

Source: Alford, Simon - Department of Biological Sciences, University of Illinois at Chicago

 

Collection: Biology and Medicine

 
56 Spinal neurons are sensitized following stimuli that activate nociceptors. This central sensitization is
 

Summary:  indicated an essential requirement for activation of 5-HT2C receptors while 5-HT1A/1B, 5-HT7 and 5-HT2A... used were 5-carboxamidotryptamine (5-CT), a 5-HT1A/1B receptor agonist; 8-hydroxy-2-(di... 5-HT2C receptor agonist (not illustrated). ...

  

Source: Hochman, Shawn - Department of Physiology, Emory University

 

Collection: Biology and Medicine

 
57 Discovery of Novel Chemotypes to a G-Protein-Coupled Receptor through Ligand-Steered Homology Modeling and Structure-Based Virtual Screening
 

Summary:  ) in feeding and energy balance, there has been considerable interest in developing MCH-R1 receptor antagonists... , a large collection of receptor-antagonist complexes were built by placing one or more known ligands... between helices 5 and 6, and the methylbenzyl ring of compound A1 is ...

  

Source: Abagyan, Ruben - School of Pharmacy and Pharmaceutical Sciences, University of California at San Diego

 

Collection: Biology and Medicine

 
58 Pharmacology of Pain edited by Pierre Beaulieu, David Lussier, Frank Porreca, and Anthony H. Dickenson
 

Summary:  as purines [26,128] (see Table I). Four subtypes of P1 receptors have been cloned--A1, A2A, A2B, and A3 (see... breakdown to ADO, it acts as a presynaptic inhibitor of transmission through P1 (A1) receptors. ATP... Receptor Main Distribution Main ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
59 P2 receptors in cardiovascular regulation and disease David Erlinge & Geoffrey Burnstock
 

Summary:  ]. Sympathetic nerves express inhibitory P2Y and P1 (A1) receptors indicating a P2 receptor-mediated negative... P2Y6 + NTPDase Ado Vasoconstriction Vasodilatation - - P1(A1) RBC ADVENTITIA CGRP SP ATP P2X P2Y ATP... . However, drugs with ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
60 UCB Pharma research day--25 October 2007 `Glia-neuron interactions and purinergic receptors
 

Summary:  . In the early 1990s, P1 and P2 receptors were cloned and characterised: four P1 receptor subtypes (A1, A2A, A2B... and in disease. For many years, it was recognised that adenosine, acting through P1 (usually A1) presynaptic... and antagonists of ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine


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61 JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION Vol. 24, No. 3, pp. 165205, 2004
 

Summary:  or antagonists at the phospholipase C-coupled receptor, whereas the drug SKF83959 has little efficacy... antagonist ligand of the Gq- and phospholipase C-coupled D1-like receptor. D1-Like Receptor Regulation of Ion... JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION Vol. ...

  

Source: Neve, Kim A. - Department of Behavioral Neuroscience, Oregon Health and Science University

 

Collection: Biology and Medicine

 
62 After the cloning of the dopamine D1 ceptors (13), several additional dopamine recep-
 

Summary:  of the substitution of a glycine (allele A2) for serine (allele A1) residue in the extracellular receptor N... , recent studies using selective competitive antagonists have shown that the dopamine D3 receptor... dopamine receptor antagonists also ...

  

Source: Brookhaven National Laboratory, Environmental Chemistry Division, Department of Applied Science

 

Collection: Environmental Sciences and Ecology

 
63 Improved docking, screening and selectivity prediction for small molecule nuclear receptor modulators using conformational
 

Summary:  ), 2aa2 (AS4), 7 S810L MR? Mineralocorticoid receptor, agonist--bound 1y9r_a (1CA), 2aa6_a (STR), 1ya3... are already targeted by known drugs, such as tamoxifen, a partial antagonist of estrogen receptor (ER... -based identification of potential nuclear receptor ...

  

Source: Abagyan, Ruben - School of Pharmacy and Pharmaceutical Sciences, University of California at San Diego

 

Collection: Biology and Medicine

 
64 TRENDS in Pharmacological Sciences Vol.22 No.4 April 2001 http://tips.trends.com 0165-6147/01/$ see front matter 2001 Elsevier Science Ltd. All rights reserved. PII: S0165-6147(00)01643-6
 

Summary:  , four subtypes of adenosine (P1) receptors were cloned [A1 , A2A , A2B and A3 (Ref. a)]. P2X receptor... Antagonists Transduction mechanisms P1 (adenosine) A1 Brain, spinal cord, testis, heart, autonomic CCPA, CPA... breakdown to adenosine, it ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
65 Contribution of Valine 70 Gating of Neuronal a3 Receptor Subtypes
 

Summary:  ). The same is true for a3b4 receptors sub- types (a3b4, 1.3 6 0.01; V70 A, 1.6 6 0.2; V70 S, 1.4 6 0.18; V70... .2; and V70 Y, 1.1 6 0.3). For a3b4 receptor subtypes, the estimated nH were (a3b4, 1.4 6 0.04; V70 A, 1.7 6... A mutation selectively increases the MLA ...

  

Source: Lasalde Dominicc, Jose A. - Department of Biology, Universidad de Puerto Rico - Rio Piedras

 

Collection: Biology and Medicine

 
66 No evidence for cross-talk between the adenosine A1 and the serotonin-1A receptor system after chronic A1 receptor
 

Summary:  Chapter 7 No evidence for cross-talk between the adenosine A1 and the serotonin-1A receptor system... after chronic A1 receptor stimulation Viktor Román, Jan N. Keijser, Paul G. M. Luiten, Peter Meerlo #12... of the adenosine ...

  

Source: Groningen, Rijksuniversiteit - Centre for Ecological and Evolutionary Studies, Department of Marine Benthic Ecology and Evolution,

 

Collection: Biology and Medicine ; Environmental Sciences and Ecology

 
67 INTERACTION BETWEEN ATP AND NERVE GROWTH FACTOR SIGNALLING IN THE SURVIVAL AND NEURITIC OUTGROWTH FROM
 

Summary:  for adenosine (A1, A2A, A2B and A3 subtypes, all G-protein-coupled) and P2 receptors for ATP (P2X ionotropic... the neuroprotective properties of A1 adenosine receptor analogues have been known for several years, the role of other... AbstractöIn a previous study we ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
68 Cellular/Molecular An Arginine Involved in GABA Binding and Unbinding But
 

Summary:  with an exponential function giving koff-SR and the per- centage of receptors occupied by antagonist at equilibrium... .Thesolidlinesarefittotheequation; percentage recovery 100 100 * [a1 exp ( IPI/ 1 ) a2 exp ( IPI/ 2 )], where a1 and 1 are the amplitude... and time ...

  

Source: Kalil, Ronald E. - Neuroscience Training Program & W.M. Keck Laboratory for Biological Imaging, University of Wisconsin at Madison; Zhang, Su-Chun - Neuroscience Training Program & Waisman Center, University of Wisconsin at Madison

 

Collection: Biology and Medicine

 
69 Neuropharmacology of alcohol addiction V Vengeliene, A Bilbao, A Molander and R Spanagel
 

Summary:  -sensitive glycine receptors. Channels Katsura et al. (2006) demonstrated an increased expression of the a1C, a1D... containing a1 seem to be more sensitive to low concentra- tions of alcohol than those containing a2 (Mihic... , the response to the ...

  

Source: Durstewitz, Daniel - Research Group Computational Neuroscience, Central Institute of Mental Health,

 

Collection: Computer Technologies and Information Sciences ; Biology and Medicine

 
70 The state of GPCR research in 2004 (20 Questions) Nat Rev Drug Discov. 2004 Jul;3(7):575, 577-626.
 

Summary:  will changing views of agonist and antagonist behaviour at GPCRs change the 588 way we view these receptors... of receptor distribution, their principal functions and agonist versus antagonist activity. Expression... receptors).Some of the first examples of such non-peptidic ...

  

Source: Sakmar, Thomas P. - Laboratory of Molecular Biology and Biochemistry, Rockefeller University

 

Collection: Biology and Medicine

 
71 doi:10.1152/ajpgi.90285.2008 295:78-87, 2008. First published May 15, 2008;Am J Physiol Gastrointest Liver Physiol
 

Summary:  -purified antibodies directed against the COOH terminus of the CB2 receptor: CB22-A (1:250, Alpha Diag- nostics, Alpha... was significantly attenuated by JWH133, whose action was reversed by the CB2 receptor antagonist AM630. Taking... control response, respectively (Fig. 1). The ...

  

Source: Buckley, Nancy E. - Biological Sciences Department, California State Polytechnic University at Pomona

 

Collection: Biology and Medicine

 
72 5-HT Receptors and the Neuromodulatory Control of
 

Summary:  ................................................................................................ 9 3.2 5-HT1A/1B receptors facilitate the induction of long-term depression... the low expression of 5-HT2A/2C receptors in the dorsal horn (see Section 2.2.2). 3.2 ...

  

Source: Hochman, Shawn - Department of Physiology, Emory University

 

Collection: Biology and Medicine

 
73 The Novel Antipsychotic Drug Lurasidone Enhances NMDA Receptor-Mediated Synaptic Responses
 

Summary:  receptors and dopamine D2 receptors. In vivo administration of the 5-HT7 receptor antagonist SB-269970... mimicked the enhancing effect of lurasidone on NMDAR responses, while the D2 receptor antagonist... receptor (NMDAR) ...

  

Source: Yan, Zhen - Department of Physiology and Biophysics, State University of New York at Buffalo

 

Collection: Biology and Medicine

 
74 5-HT2A Receptor-Mediated Regulation of Brain-Derived Neurotrophic Factor mRNA in the Hippocampus and the Neocortex
 

Summary:  with a selective 5-HT2A, but not 5-HT2C, receptor antagonist. The expression of BDNF mRNA in the hippocampus... . Pretreatment with ketan- serin, a 5-HT2A/2C receptor antagonist, significantly blocked the stress... treatment. For the receptor antagonists experiments, ...

  

Source: Vaidya, Vidita - Department of Biological Sciences, Tata Institute of Fundamental Research

 

Collection: Biology and Medicine

 
75 BI-DIRECTIONAL MODULATION OF BED NUCLEUS OF STRIA TERMINALIS NEURONS BY 5-HT: MOLECULAR EXPRESSION AND
 

Summary:  receptor antagonist, WAY 100635 (200 nM) evoked only a monophasic inward current (Fig. 2A) with a reversal... is not a selective 5-HT2 receptor antagonist Fig. 2. Monophasic inward current to 5-HT unmasked by the 5-HT1A... . Consequently, we next examined the ability of more selective 5-HT ...

  

Source: Rainnie, Donald "Tig" - Yerkes National Primate Research Center, Emory University

 

Collection: Biology and Medicine

 
76 2001 Wiley-Liss, Inc. DRUG DEVELOPMENT RESEARCH 52:110 (2001)
 

Summary:  were cloned, namely, A1, A2A, A2B, and A3 [Ralevic and Burnstock, 1998]. P2X Receptor Family P2X... :246­254. Vainio M, Törnquist K. 2000. The role of adenosine A1 receptors in the ATP-evoked Ca2+ response in rat... ,-methylene ATP (,-meATP), and there are now very ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
77 Neuropharmacology 43 (2002) 13131323 www.elsevier.com/locate/neuropharm
 

Summary:  subdivisions of P1 recep- tors, into A1, A2A, A2B and A3 and of P2 receptors into P2X and P2Y families... responses were inhibited by the P2Y1-selective antagonist MRS 2179, and suramin. P2Y1 receptors were... antagonists, immunostain- ing and in situ hybridization ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
78 Z .European Journal of Pharmacology 342 1998 325332 Mechanism of the dynorphin-induced dualistic effect on free intracellular
 

Summary:  induced by a high concentration of dynorphin A- 1­ .17 , implying that the k-opioid receptor is implicated... Z .the paralytic effect of dynorphin A- 1­17 and dynorphin Z .A- 2­17 but the non-NMDA receptor... concentrations of dynorphin A- ...

  

Source: Hu, Wen-Hui - Department of Physiology, Virginia Commonwealth University

 

Collection: Biology and Medicine

 
79 Journal of Steroid Biochemistry & Molecular Biology 88 (2004) 351360 Identification of novel estrogen receptor antagonists
 

Summary:  estrogen receptor antagonists Dalei Shaoa,, Thomas J. Berrodina, Eric Manasb, Diane Hauzeb, Robert Powersc... receptor alpha (ER ) antagonists using both cell-based and computer-based virtual screening strategies... ; Coactivators; SRC; Antagonist 1. Introduction Estrogen ...

  

Source: Powers, Robert - Department of Chemistry, University of Nebraska-Lincoln

 

Collection: Chemistry

 
80 81:925-929, 1999.J Neurophysiol M. R. Foy, J. Xu, X. Xie, R. D. Brinton, R. F. Thompson and T. W. Berger
 

Summary:  by 17 -estradiol perfusion of pharmacologically isolated non-NMDA receptor-mediated EPSPs. A: 1 nM 17... -phosphonovalerate [D- APV, a competitive N-methyl-D-aspartate (NMDA) receptor antagonist] supported a postsynaptic... steroids can be blocked by an NMDA receptor ...

  

Source: Brinton, Roberta Diaz - Laboratory for Neuroscience Research & School of Pharmacy, University of Southern California

 

Collection: Biology and Medicine


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81 BIOLOGY COLLOQUIUM Monday, October 31, 2011
 

Summary:  weeks (flare effect) followed by an overall antagonist effect resulting from receptor down... and can lead to increased side-effects such as lower bone density. A full receptor antagonist is expected... on a campaign to discover small molecule antagonists of the GnRH ...

  

Source: Heller, Barbara - Department of Applied Mathematics, Illinois Institute of Technology

 

Collection: Mathematics

 
82 Fax +41 61 306 12 34 E-Mail karger@karger.ch
 

Summary:  .1 µM 1 µM 3 µM 10 µm 100 µM 100 pA 1 s a b c d Recording electrode Normalizedresponse 1.0 0.8 0.6 0... 31.3 ms. Deactivation of the re- 100 µM GABA BIC GABA + BIC 50 pA 1 s 50 pA 1 s 0 µM 100 µM GABA 100... µM GABA 100 µM BIC 1 µM 10 µM 100 µM 100 ...

  

Source: Liu, Jian - Harvard University

 

Collection: Biology and Medicine

 
83 Augmentation of the Neurochemical and Behavioural Effects of SSRIs
 

Summary:  shown that 5-HT2A receptor increases cAMP in A1A1 adrenal cells by the intermediary action of calmodulin... of the SSRI, citalopram, in combination with a number of monoamine receptor agonists and antagonists... are tryptamine derivatives or ...

  

Source: Groningen, Rijksuniversiteit - Centre for Ecological and Evolutionary Studies, Department of Marine Benthic Ecology and Evolution,

 

Collection: Biology and Medicine ; Environmental Sciences and Ecology

 
84 Purinergic signalling *Geoffrey Burnstock
 

Summary:  /ADP, respectively, was proposed (Burnstock, 1978). Four subtypes of P1 receptors have been cloned, namely A1, A2A, A... for (a) 1/s and (b) 30/s. Upper trace tension, and lower trace membrane potential. Note the phase... ATP receptor antagonists ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
85 Behavioral/Systems/Cognitive Role of Neurokinin 3 Receptors in Supraoptic Vasopressin
 

Summary:  ) are expressed in the supraoptic nucleus (SON), and SON is innervated by substance P (SP)-expressing A1 neurons... , and (2) stimulation of the A1 pathway by hypotension activates SON NK3-Rs. Senktide, an NK3-R agonist... , stimulated VP release from HNS explants, but neither a neurokinin 1 ...

  

Source: Betz, William J. - Department of Physiology and Biophysics, University of Colorado Health Sciences Center

 

Collection: Biology and Medicine

 
86 DOI: 10.1126/science.1146317 , 815 (2007);318Science
 

Summary:  .sciencemag.orgDownloadedfrom #12;TARP Auxiliary Subunits Switch AMPA Receptor Antagonists into Partial Agonists Karen Menuz,1... (AMPA) receptor antagonists. However, we find that in the presence of transmembrane AMPA receptor... receptor ...

  

Source: Stroud, Robert - Department of Biochemistry and Biophysics, University of California at San Francisco

 

Collection: Biology and Medicine

 
87 Microscopic Kinetics and Energetics Distinguish GABAA Receptor Agonists from Antagonists
 

Summary:  Microscopic Kinetics and Energetics Distinguish GABAA Receptor Agonists from Antagonists Mathew V... and unbinding kinetics of GABAA receptor agonists and antagonists in outside-out patches from rat hippocampal... after each experiment. GABAA receptor agonists and ...

  

Source: Kalil, Ronald E. - Neuroscience Training Program & W.M. Keck Laboratory for Biological Imaging, University of Wisconsin at Madison

 

Collection: Biology and Medicine

 
88 PERSPECTIVE Orphan nuclear receptors--new ligands
 

Summary:  steroid receptors. Prominently inducible members of the rodent P450 3A gene family (CYP3A1, CYP3A2, CYP3A... - tochrome P-450 3A1 by dexamethasone and the antigluco- New orphan receptor ligands GENES & DEVELOPMENT 3153... , spironolactone, cyproterone acetate) are ...

  

Source: Blumberg, Bruce - Department of Developmental and Cell Biology, University of California, Irvine

 

Collection: Biology and Medicine

 
89 Z .European Journal of Pharmacology 405 2000 7388 www.elsevier.nlrlocaterejphar
 

Summary:  receptor within a1 circumscribed time window yielded greater potentiation than simultaneous exposure... of potentiation.1 Pre-exposure of vasopressin V receptor agonist for 60 s resulted in a1 75% potentiation... -induced potentiation was blocked by a vasopressin V ...

  

Source: Brinton, Roberta Diaz - Laboratory for Neuroscience Research & School of Pharmacy, University of Southern California

 

Collection: Biology and Medicine

 
90 GABAA Receptor 2 Tyr97 Line the GABA-binding Site
 

Summary:  -maximal response for each receptor (44, 45). MTS Reactions and Agonist/Antagonist Protection Assays... 1 2(V93C) 3.8 1.3 1.24 0.02 3 2.4 0.05 0.002a 0.99 0.09 4 0.2 1 2(P94C) 35.1 4.3a 1.16 0.20 3 22 0... .11 0.01a 0.96 0.14 3 0.3 1 2(D95C) 54.9 13.6a 1.43 0.20 3 34 ...

  

Source: Jackson, Meyer B. - Neuroscience Training Program & Department of Physiology, University of Wisconsin at Madison; Kalil, Ronald E. - Neuroscience Training Program & W.M. Keck Laboratory for Biological Imaging, University of Wisconsin at Madison

 

Collection: Biology and Medicine

 
91 Presynaptic Nicotinic Receptors Facilitate Monoaminergic Transmission
 

Summary:  by the 5-HT1A antagonist pindobind-5-HT1A (1 M; n 6; Fig. 3D). In addition, the pindobind-sensitive current... by the observation that they were blocked by a nicotinic receptor antagonist, mecamylamine (50 M; n 4; Fig. 1C... additional nicotinic receptor ...

  

Source: Rainnie, Donald "Tig" - Yerkes National Primate Research Center, Emory University

 

Collection: Biology and Medicine

 
92 Mapping convulsants' binding to the GABA-A receptor chloride ionophore: A proposed model for channel binding sites
 

Summary:  to eight families: a1­6, b1­3, g1­3, d, e, p, u and r1­3) around the ionophore (Baumann et al., 2001, 2002... from antagonist into allosteric potentiator. Given similarity of various ionophore receptors... .L., Machu, T.K., Dillon, G.H., 2003. The GABA(A) receptor ...

  

Source: Kalueff, Allan V. - Department of Pharmacology, Tulane University

 

Collection: Biology and Medicine

 
93 Research Article Northern Ring Conformation of Methanocarba-Adenosine
 

Summary:  at the hP2Y4 receptor this compound has weak agonist activity. In contrast, ATP is an antagonist at the P2Y... investigated the ability of this compound to act as an antagonist at the P2X2/3 receptor. In these experiments... 2340 3 µM MRS 2312 3 µM ATP 3 µM 0.5 nA ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
94 The influence of hypothermia on P2 receptor-mediated responses of frog skeletal muscle
 

Summary:  -cyclopentylxantine (DPCPX), a selective adeno- sine A1 receptor antagonist, abolishes the inhibitory action... of Pharmacology 509 (2005) 187­193 191 #12;was shown that in guinea-pig tissues, adenosine A1 receptor... that presynaptic P1 ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
95 Behavioral/Systems/Cognitive Conversion of the Modulatory Actions of Dopamine on
 

Summary:  . In contrast, the highly selective D3 receptor selective antagonists GR 103691 and nafadotride (both from... of both MSR and the longer- latency reflexes were similar between WT and D3KO mice (Fig. 2A1,A2). A rank... to a decrease in the MSR amplitudes (Fig. 3A1). ...

  

Source: Hochman, Shawn - Department of Physiology, Emory University

 

Collection: Biology and Medicine

 
96 Neuropharmacology 47 (2004) 10931101 www.elsevier.com/locate/neuropharm
 

Summary:  were blocked by the selective A1 receptor antagonist, DPCPX. TNP-ATP and PPADS reduced distension... and DPCPX (30 lM), an A1 receptor antagonist, was able to completely block the ATP-evoked effects. DPCPX... of the slow ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
97 Pharmacological properties of P2 receptors on rat otic parasympathetic ganglion neurons
 

Summary:  with the Hill equation: Y=A/[1+(K/X)nH ], where A is the maximum effect, K is the EC50 and nH is the Hill... . 2). Antagonists TNP-ATP is a selective antagonist on rP2X1, rP2X3 and rP2X2/3 receptors relative... -selective P2 receptor antagonists ...

  

Source: Burnstock, Geoffrey - Autonomic Neuroscience Centre, University College London

 

Collection: Biology and Medicine

 
98 An aplysia dopamine1-like receptor: molecular and functional characterization
 

Summary:  , with an EC50 of 155 nM (Fig. 5b). As a control, methiothepin, a selective 5-HT receptor antagonist... % of the response was calculated. Flupentixol (a mixed D1/D2 dopamine receptor antagonist) and, surprisingly... , methiothe- pin (a 5-HT receptor antagonist) were the ...

  

Source: Byrne, John H. - Department of Neurobiology and Anatomy, University of Texas Medical School at Houston

 

Collection: Biology and Medicine

 
99 Behaioural Pharmacology 2001; 00:1 10 REVIEW Serotonin receptors in mood disorders: a combined1A
 

Summary:  of cocaine by 5-HT receptors: a1B comparison of knockouts and antagonists. Pharmacol Biochem ( )Beha¨ 67 3... lines of evidence point towards the Z .serotonin 5-HT receptor as a putative key1A 1A player... genetic manip- ulations of the 5-HT ...

  

Source: Sibille, Etienne - Center for the Neural Basis of Cognition & Department of Psychiatry, University of Pittsburgh

 

Collection: Biology and Medicine

 
100 Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons
 

Summary:  Antonio, U.S.A. 1 The prototypical aminoalkylindole cannabinoid WIN 55,212-2 (WIN-2) has been shown... ruthenium red but not by the vanilloid receptor type 1 (TRPV1) antagonist capsazepine, suggesting that... was not reversed by antagonists of cannabinoid type 1 (CB1) ...

  

Source: Price, Theodore - Department of Pharmacology, University of Arizona

 

Collection: Biology and Medicine


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