[A comparative study of the neurochemical profiles of carbidine stereoisomers].
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.
Gaĭnetdinov
R R
RR
Miroshnichenko
I I
II
Kudrin
V S
VS
Bogdanov
M B
MB
Pogorelov
V M
VM
Budygin
E A
EA
Kovalev
G I
GI
Raevskiĭ
K S
KS
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
D014150:Antipsychotic Agents; D002243:Carbolines; D004295:Dihydroxyphenylalanine; D004298:Dopamine; C100106:dicarbine
Sravnitel'noe izuchenie neĭrokhimicheskikh profileĭ stereoizomerov karbidina.