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Titolo:
In vivo neurobiological effects of ibogaine and its O-desmethyl metabolite, 12-hydroxyibogamine (noribogaine), in rats
Autore:
Baumann, MH; Rothman, RB; Pablo, JP; Mash, DC;
Indirizzi:
NIDA, Clin Psychopharmacol Sect, Intramural Res Program, NIH, Baltimore, MD 21224 USA NIDA Baltimore MD USA 21224 ral Res Program, NIH, Baltimore, MD 21224 USA Univ Miami, Sch Med, Dept Neurol, Miami, FL USA Univ Miami Miami FL USAUniv Miami, Sch Med, Dept Neurol, Miami, FL USA
Titolo Testata:
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
fascicolo: 2, volume: 297, anno: 2001,
pagine: 531 - 539
SICI:
0022-3565(200105)297:2<531:IVNEOI>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
INDUCED LOCOMOTOR-ACTIVITY; NUCLEUS-ACCUMBENS; ALKALOID IBOGAINE; SEROTONIN; MORPHINE; DOPAMINE; BRAIN; FENFLURAMINE; MECHANISMS; IDENTIFICATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
43
Recensione:
Indirizzi per estratti:
Indirizzo: Baumann, MH NIDA, Clin Psychopharmacol Sect, Intramural Res Program, NIH, 5500 Nathan Shock Dr, Baltimore, MD 21224 USA NIDA 5500 Nathan Shock Dr Baltimore MD USA 21224 MD 21224 USA
Citazione:
M.H. Baumann et al., "In vivo neurobiological effects of ibogaine and its O-desmethyl metabolite, 12-hydroxyibogamine (noribogaine), in rats", J PHARM EXP, 297(2), 2001, pp. 531-539

Abstract

Ibogaine is a naturally occurring compound with purported antiaddictive properties. When administered to primates, ibogaine is rapidly o-demethylatedto form the metabolite 12-hydroxyibogamine (noribogaine). Peak blood levels of noribogaine exceed those of ibogaine, and noribogaine persists in the bloodstream for at least 1 day. Very few studies have systematically evaluated the neurobiological effects of noribogaine in vivo. In the present series of experiments, we compared the effects of i.v. administration of ibogaine and noribogaine (1 and 10 mg/kg) on motor behaviors, stress hormones, and extracellular levels of dopamine (DA) and serotonin (5-HT) in the nucleusaccumbens of male rats. Ibogaine caused dose-related increases in tremors,whereas noribogaine did not. Both ibogaine and noribogaine produced significant elevations in plasma corticosterone and prolactin, but ibogaine was amore potent stimulator of corticosterone secretion. Neither drug altered extracellular DA levels in the nucleus accumbens. However, both drugs increased extracellular 5-HT levels, and noribogaine was more potent in this respect. Results from in vitro experiments indicated that ibogaine and noribogaine interact with 5-HT transporters to inhibit 5-HT uptake. The present findings demonstrate that noribogaine is biologically active and undoubtedly contributes to the in vivo pharmacological profile of ibogaine in rats. Noribogaine is approximately 10 times more potent than ibogaine as an indirect 5-HT agonist. More importantly, noribogaine appears less apt to produce theadverse effects associated with ibogaine, indicating the metabolite may bea safer alternative for medication development.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 07:29:55