Stereoisomers of the atypical neuroleptic carbidine modulate striatal dopamine release in awake rats.
Intracerebral microdialysis was used to monitor extracellular levels of dopamine (DA), 3,4-dihydroxyphenylacetic acid and homovanillic acid in awake rats, after intraperitoneal administration of the cis- and trans-isomers (25 mg/kg and 1 mg/kg, respectively) of carbidine, the atypical neuroleptic drug, in comparison with sulpiride (50 mg/kg) and haloperidol (1 mg/kg). Trans-carbidine was found to be more potent than the cis-isomer in increasing the release of DA. In contrast to sulpiride and haloperidol, both isomers at the doses used, produced only a moderate elevation in the levels of the metabolites of DA. Transcarbidine seemed to be more potent as a neuroleptic drug, in comparison with the cis-isomer.
Department of Neuropsychopharmacology, USSR Academy of Medical Sciences, Moscow.
R R
RR
Guinetdinov
M B
MB
Bogdanov
V M
VM
Pogorelov
V S
VS
Kudrin
K S
KS
Rayevsky
D015102:3,4-Dihydroxyphenylacetic Acid / Q000378:metabolism; D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D002243:Carbolines / Q000494:pharmacology*; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D003956:Dialysis / Q000379:methods; D004298:Dopamine / Q000378:metabolism*; D006220:Haloperidol / Q000494:pharmacology; D006719:Homovanillic Acid / Q000378:metabolism; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D013469:Sulpiride / Q000494:pharmacology
D014150:Antipsychotic Agents; D002243:Carbolines; D015102:3,4-Dihydroxyphenylacetic Acid; D013469:Sulpiride; D006220:Haloperidol; D004298:Dopamine; D006719:Homovanillic Acid; C100106:dicarbine