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Titolo:
PHARMACOLOGICAL EFFECTS OF EPIBATIDINE OPTICAL ENANTIOMERS
Autore:
DAMAJ MI; CREASY KR; GROVE AD; ROSECRANS JA; MARTIN BR;
Indirizzi:
VIRGINIA COMMONWEALTH UNIV,MED COLL VIRGINIA,DEPT PHARMACOL & TOXICOLRICHMOND VA 23298 VIRGINIA COMMONWEALTH UNIV,MED COLL VIRGINIA,DEPT PHARMACOL & TOXICOLRICHMOND VA 23298
Titolo Testata:
Brain research
fascicolo: 1-2, volume: 664, anno: 1994,
pagine: 34 - 40
SICI:
0006-8993(1994)664:1-2<34:PEOEOE>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
NICOTINE-INDUCED ANTINOCICEPTION; MORPHINE; BINDING; MICE;
Keywords:
EPIBATIDINE; NICOTINE; ANTINOCICEPTION; DRUG DISCRIMINATION; LOCOMOTOR ACTIVITY; HYPOTHERMIA;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
M.I. Damaj et al., "PHARMACOLOGICAL EFFECTS OF EPIBATIDINE OPTICAL ENANTIOMERS", Brain research, 664(1-2), 1994, pp. 34-40

Abstract

The pharmacology of synthetic D- and L-epibatidine, an alkaloid originally characterized from frog skin, were studied in different behavioral tests in mice and rats. The two enantiomers have potent antinociceptive activity in mice using the tail-flick test, with an ED(50) of 6.1and 6.6 mu g/kg for L- and D-epibatidine respectively. Epibatidine enantiomers were 200 X more potent than L-nicotine as an antinociceptiveagent in mice after s.c. administration. Their analgesic effect was blocked by mecamylamine but not naloxone, an opiate antagonist. Both D-and L-epibatidine have high affinity (K-i 54.7 and 55.0 pM, respectively) for [H-3]nicotine binding site in rat brain. In addition, they reduced mice locomotor activity and body temperature in a dose-dependentmanner. In rats trained with nicotine (0.4 mg/kg), epibatidine enantiomers engendered nicotine-like responding in a dose-related manner with an ED(50) of 1.00 and 0.93 mu g/kg for D and L, respectively. The discriminative effect of L- and D-epibatidine in rats was blocked by mecamylamine but not by hexamethonium. As in binding results, there was no significant enantioselectivity for these effects in our study.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/09/20 alle ore 21:36:38