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Titolo:
ERYSODINE, A COMPETITIVE ANTAGONIST AT NEURONAL NICOTINIC ACETYLCHOLINE-RECEPTORS
Autore:
DECKER MW; ANDERSON DJ; BRIONI JD; DONNELLYROBERTS DL; KANG CH; ONEILL AB; PIATTONIKAPLAN M; SWANSON S; SULLIVAN JP;
Indirizzi:
ABBOTT LABS,DEPT 47W,DIV PHARMACEUT PROD,BLDG AP-9A-LL,100 ABBOTT PK RD ABBOTT PK IL 60064
Titolo Testata:
European journal of pharmacology
fascicolo: 1, volume: 280, anno: 1995,
pagine: 79 - 89
SICI:
0014-2999(1995)280:1<79:EACAAN>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
ELEVATED PLUS-MAZE; RAT-BRAIN; CHOLINERGIC RECEPTOR; ALPHA-BUNGAROTOXIN; BINDING-SITES; BLOCKADE; CHLORISONDAMINE; AGONISTS; LIGAND;
Keywords:
NICOTINIC ACETYLCHOLINE RECEPTOR ANTAGONIST; ERYSODINE; DIHYDRO-BETA-ERYTHROIDINE; PHARMACOKINETICS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
M.W. Decker et al., "ERYSODINE, A COMPETITIVE ANTAGONIST AT NEURONAL NICOTINIC ACETYLCHOLINE-RECEPTORS", European journal of pharmacology, 280(1), 1995, pp. 79-89

Abstract

Erysodine, an erythrina alkaloid related to dihydro-beta-erythroidine, was found to be a more potent inhibitor of [H-3]cytisine binding at neuronal nicotinic acetylcholine receptors but a less potent inhibitorof [I-125]alpha-bungarotoxin binding at muscle-type nicotinic acetylcholine receptors than dihydro-beta-erythroidine. Erysodine was a competitive, reversible antagonist of (-)-nicotine-induced dopamine releasefrom striatal slices and inhibited (-)-nicotine-induced Rb-86(+) efflux from IMR-32 cells. Erysodine was equipotent with dihydro-beta-erythroidine in the dopamine release assay but 10-fold more potent in the Rb-86(+) efflux assay, suggesting differential subtype selectivity for these two antagonists. Erysodine, systemically administered to mice, entered the brain and significantly attentuated nicotine's hypothermic effects and its anxiolytic-like effects in the elevated plus-maze test. There was greater separation between antagonist and toxic doses for erysodine than for dihydro-beta-erythroidine, perhaps because of erysodine's greater selectivity for neuronal receptors. In rats, erysodine prevented both the early developing decrease and the late-developing increase in locomotor activity produced by (-)-nicotine. The potent andcompetitive nature of erysodine's antagonism together with its ability to enter the brain after systemic administration suggest that erysodine may be a useful tool in characterizing neuronal nicotinic acetylcholine receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 02:45:50