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Characterization of the muscarinic cholinoceptors in the human detrusor

Journal Article · · J. Urol.; (United States)
OSTI ID:5021745
; ;
Contractions of the human detrusor are thought to be mediated mainly via cholinergic muscarinic receptors. In the present study, the authors used a receptor-binding technique with 1-quinuclidinyl(phenyl 4-/sup 3/H)benzilate ((-)/sup 3/H-QNB) as radioligand to directly demonstrate the presence of muscarinic receptors in homogenates of the human detrusor. The binding of (-)/sup 3/H-QNB was of high affinity (KD = (1.2 +/- 0.1) X 10(-10) M), saturable (Ro = 160 +/- 15 fmol./mg. protein) and possessed the pharmacological specificity expected of an interaction with muscarinic receptors. Muscarinic receptor antagonists were bound to a virtually uniform population of sites, whereas muscarinic receptor agonists recognized more than one population of muscarinic binding sites. The affinities of a series of antimuscarinic drugs, determined in competition experiments with (-)/sup 3/H-QNB, were found to correlate with the capacity to inhibit carbachol-induced contractions in isolated human bladder muscle. Binding data together with the functional data indicated that the human detrusor does not contain any significant number of muscarinic spare receptors. The results suggest that a selective effect on the muscarinic receptors of human bladder is not possible to obtain with presently available antimuscarinic agents.
Research Organization:
KabiVitrum AB, Stockholm, Sweden
OSTI ID:
5021745
Journal Information:
J. Urol.; (United States), Journal Name: J. Urol.; (United States) Vol. 2; ISSN JOURA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ACETYLCHOLINE
AFFINITY
AMINES
AMMONIUM COMPOUNDS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BENZILIC ACID
BIOCHEMICAL REACTION KINETICS
BLADDER
BODY
CARBOXYLIC ACIDS
DRUGS
ESTERS
HYDROXY ACIDS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MAN
MUSCLES
NEUROREGULATORS
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANS
PARASYMPATHOLYTICS
PARASYMPATHOMIMETICS
PRIMATES
QUATERNARY COMPOUNDS
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
URINARY TRACT
VERTEBRATES