Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
STRUCTURE-ACTIVITY-RELATIONSHIPS FOR MECAMYLAMINES ANTAGONISM OF NICOTINE IN THE CENTRAL-NERVOUS-SYSTEM
Autore:
CREASY KR; DAMAJ MI; DIMEN KR; GLASSCO WS; MAY EL; MARTIN BR;
Indirizzi:
VIRGINIA COMMONWEALTH UNIV,MED COLL VIRGINIA,DEPT PHARMACOL & TOXICOLRICHMOND VA 23298
Titolo Testata:
Medicinal chemistry research
fascicolo: 7-8, volume: 6, anno: 1996,
pagine: 535 - 542
SICI:
1054-2523(1996)6:7-8<535:SFMAON>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN MEMBRANES; MOUSE-BRAIN; BINDING; ACETYLCHOLINE; SITES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
22
Recensione:
Indirizzi per estratti:
Citazione:
K.R. Creasy et al., "STRUCTURE-ACTIVITY-RELATIONSHIPS FOR MECAMYLAMINES ANTAGONISM OF NICOTINE IN THE CENTRAL-NERVOUS-SYSTEM", Medicinal chemistry research, 6(7-8), 1996, pp. 535-542

Abstract

Although mecamylamine antagonizes many of nicotine's effects in the central nervous system (CNS), the mechanism by which this antagonism occurs is not yet fully understood. We studied the in vivo responses of various mecamylamine analogs to determine the existence of structure-activity relationships. Doses which produced 50% antagonism (AD(50)) inthe presence of an ED(84) of nicotine were calculated for the analogsin both the tail-flick and spontaneous activity tests. It was found that the amine position yields optimal in vivo activity when joined to a single methyl substituent, as is the case with mecamylamine; the addition of larger substituents decreases activity. This was especially true in the case of the tail-flick test. N-Benzyl mecamylamine displayspoor antagonist activity while N-(4-fluoro) and N-(4-nitrobenzyl) mecamylamine seem totally inactive. Furthermore, [H-3]nicotine binding was not displaced in vine by mecamylamine analogs. Based on pharmacological data such as this, it appears that mecamylamine's mechanism of action in the CNS is distinct from that of nicotine and may not be mediated by the same population of receptors to which nicotine binds.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/09/20 alle ore 09:40:02