The releasing effect of the isomers of the alkaloid cathinone at central and peripheral catecholamine storage sites.
The alkaloid (-)cathinone is known to have an amphetamine-like releasing effect on physiological storage sites for catecholamines. The present study was performed in order to determine whether the synthetic enantiomer (+)cathinone would have a comparable effect. This was done by measuring the release of radioactivity in response to the cathinone isomers, from tissue slices taken from different areas of the nervous system of the rat and prelabelled with tritiated catecholamines ([3H]dopamine: nucleus accumbens and nucleus caudatus; [3H]noradrenaline: atrium and vas deferens). The two isomers of cathinone were found to be approximately equipotent in inducing release at peripheral noradrenergic nerve endings, but the (-)isomer was about three times more potent than the (+)isomer at dopamine terminals in the CNS. Thus, the releasing effect of the cathinones is characterized by a certain degree of stereoselectivity with regard to dopamine storage sites in the CNS, but not with regard to peripheral noradrenergic nerve endings.
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002395:Catecholamines / Q000378:metabolism*; D003342:Corpus Striatum / Q000378:metabolism; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009206:Myocardium / Q000378:metabolism; D009714:Nucleus Accumbens / Q000378:metabolism; D009830:Olfactory Bulb / Q000378:metabolism; D011619:Psychotropic Drugs / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D014649:Vas Deferens / Q000187:drug effects
D000470:Alkaloids; D002395:Catecholamines; D011619:Psychotropic Drugs; C023665:cathinone