Further evidence for an amphetamine-like mechanism of action of the alkaloid cathinone. 1986

P Kalix, and R A Glennon

The alkaloid (-)cathinone is a potent stimulant with pharmacological properties closely resembling those of (+)amphetamine. Since (-)cathinone is capable of inducing release at physiological catecholamine storage sites, it has been suggested that (-)cathinone and (+)amphetamine have the same mechanism of action. In the present study, the potency of (-)cathinone in inducing the release of radioactivity from 3H-dopamine prelabelled tissue of the rat caudate nucleus was compared to that of several structural analogs, i.e. to that of four other aminophenones. (-)Cathinone was found to be the most potent of the compounds under investigation, and among these only demethylcathinone had an effect that was within the same order of magnitude as that of (-)cathinone. Furthermore, (-)cathinone and two of its analogs were evaluated in behavioral experiments with regard to their ability to substitute for (+)amphetamine in rats trained to discriminate between (+)amphetamine and saline. It was found that, unlike the other aminophenones, (-)cathinone is capable of producing (+)amphetamine-like stimulus effects, and these can be antagonized by haloperidol in a dose-related manner. Taken together, these findings support the hypothesis that (+)amphetamine and (-)cathinone produce their central stimulant effect via the same dopaminergic mechanism.

UI MeSH Term Description Entries
D002421 Caudate Nucleus Elongated gray mass of the neostriatum located adjacent to the lateral ventricle of the brain. Caudatus,Nucleus Caudatus,Caudatus, Nucleus,Nucleus, Caudate
D004298 Dopamine One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action. Hydroxytyramine,3,4-Dihydroxyphenethylamine,4-(2-Aminoethyl)-1,2-benzenediol,Dopamine Hydrochloride,Intropin,3,4 Dihydroxyphenethylamine,Hydrochloride, Dopamine
D006220 Haloperidol A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) Haldol
D000470 Alkaloids Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed) Alkaloid,Plant Alkaloid,Plant Alkaloids,Alkaloid, Plant,Alkaloids, Plant
D000662 Amphetamines Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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