7-(3-(4-(2,3-dimethylphenyl)piperazinyl)propoxy)-2 (1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist
Journal Article
·
· Life Sci.; (United States)
The assertion that OPC-4392 acts as an agonist at presynaptic dopamine autoreceptors is supported by the following behavioral and biochemical observations: OPC-4392, 3-PPP and apomorphine inhibited the reserpine-induced increase in DOPA accumulation in the forebrain of mice and in the frontal cortex, limbic forebrain and striatum of rats. In addition, the gamma-butyrolactone (GBL)-induced increase in DOPA accumulation in the mouse forebrain was also inhibited by OPC-4392, 3-PPP and apomorphine. The inhibitory effect of OPC-4392 on GBL-induced DOPA accumulation lasted for at least 8 hours after oral administration to mice, while that of 3-PPP and apomorphine disappeared in 4 hours after subcutaneous injection. OPC-4392 failed to increase spontaneous motor activity in reserpinized mice, enhance spontaneous ipsilateral rotation in rats with unilateral striatal kainic acid (KA) lesions, induce contralateral rotation in rats with unilateral striatal 6-hydroxydopamine (6-OHDA) lesions and inhibit /sup 14/C-acetylcholine (Ach) release stimulated by 20 mM KCl in rat striatal slices.
- Research Organization:
- Otsuka Pharmaceutical Co., Ltd., Tokushima (Japan)
- OSTI ID:
- 5210147
- Journal Information:
- Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 42:20; ISSN LIFSA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ACETYLCHOLINE
AMINES
AMMONIUM COMPOUNDS
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZINES
BIOLOGICAL FUNCTIONS
BIOSYNTHESIS
BODY
BRAIN
CARBON 14 COMPOUNDS
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
DOPAMINE
DRUGS
ESTERS
FUNCTIONS
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INHIBITION
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
MICE
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PARASYMPATHOMIMETICS
PHENOLS
POLYPHENOLS
PROTEINS
PYRIDINES
QUATERNARY COMPOUNDS
QUINOLINES
RATS
RECEPTORS
RODENTS
SYMPATHOMIMETICS
SYNTHESIS
TRACER TECHNIQUES
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
ACETYLCHOLINE
AMINES
AMMONIUM COMPOUNDS
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZINES
BIOLOGICAL FUNCTIONS
BIOSYNTHESIS
BODY
BRAIN
CARBON 14 COMPOUNDS
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
DOPAMINE
DRUGS
ESTERS
FUNCTIONS
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INHIBITION
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
MICE
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PARASYMPATHOMIMETICS
PHENOLS
POLYPHENOLS
PROTEINS
PYRIDINES
QUATERNARY COMPOUNDS
QUINOLINES
RATS
RECEPTORS
RODENTS
SYMPATHOMIMETICS
SYNTHESIS
TRACER TECHNIQUES
VERTEBRATES