title: [A comparative study of the neurochemical profiles of carbidine stereoisomers].
abstract: The effects of cis- and trans-isomers of atypical neuroleptic carbidine on the synthesis of dopamine and its autoreceptor regulation in the striatum and nucleus accumbens of rats were examined by blocking decarboxylase of L-aromatic amino acids and interrupting the nerve impulse flow in the dopaminergic neurons. The striatal release and metabolism of dopamine were studied in vitro by employing K(+)-stimulated efflux from isolated striata and in vivo by the microdialysis in freely moving rats. Carbidine trans-isomer, unlike its cis-isomer, was shown to enhance the biosynthesis of dopamine via blockade of presynaptic autoreceptors presumably located on the dopaminergic terminals. The trans-isomer was found to be much more potent by affecting the neurochemical parameters of dopaminergic neurotransmission, which are essential for the drug to produce its antipsychotic effect.
authors.forename: R R
authors.initials: RR
authors.lastname: Gaĭnetdinov
authors.forename: I I
authors.initials: II
authors.lastname: Miroshnichenko
authors.forename: V S
authors.initials: VS
authors.lastname: Kudrin
authors.forename: M B
authors.initials: MB
authors.lastname: Bogdanov
authors.forename: V M
authors.initials: VM
authors.lastname: Pogorelov
authors.forename: E A
authors.initials: EA
authors.lastname: Budygin
authors.forename: G I
authors.initials: GI
authors.lastname: Kovalev
authors.forename: K S
authors.initials: KS
authors.lastname: Raevskiĭ
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000737:chemistry* / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002243:Carbolines / Q000737:chemistry* / Q000494:pharmacology; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D004295:Dihydroxyphenylalanine / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D013997:Time Factors
chemical_list: D014150:Antipsychotic Agents; D002243:Carbolines; D004295:Dihydroxyphenylalanine; D004298:Dopamine; C100106:dicarbine
vernacular_title: Sravnitel'noe izuchenie neĭrokhimicheskikh profileĭ stereoizomerov karbidina.