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Titolo:
Synthesis and in vivo and in vitro evaluation isoarecolone and derivatives
Autore:
Beach, JW; Damaj, MI; Jonnala, RR; Terry, AV; Buccafusco, JJ;
Indirizzi:
UnivAGeorgia, Coll Pharm, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 US Univ Georgia Athens GA USA 30602 maceut & Biomed Sci, Athens, GA 30602 US Univ Georgia, Coll Pharm, Dept Clin & Adm Sci, Athens, GA 30602 USA Univ Georgia Athens GA USA 30602 ept Clin & Adm Sci, Athens, GA 30602 USA Virginiachmond,wealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Ri Virginia Commonwealth Univ Richmond VA USA 23298 Pharmacol & Toxicol, Ri Med Coll Georgia, Alzheimers Res Ctr, Dept Pharmacol & Toxicol, Augusta, GA Med Coll Georgia Augusta GA USA 30912 pt Pharmacol & Toxicol, Augusta, GA
Titolo Testata:
MEDICINAL CHEMISTRY RESEARCH
fascicolo: 9, volume: 8, anno: 1998,
pagine: 510 - 522
SICI:
1054-2523(1998)8:9<510:SAIVAI>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
NICOTINIC-CHOLINERGIC RECEPTORS; ACETYLCHOLINE-RECEPTORS; ALPHA-BUNGAROTOXIN; DOPAMINE RELEASE; RAT-BRAIN; PHARMACOLOGICAL CHARACTERIZATION; BETA-SUBUNITS; H-3 NICOTINE; MOUSE-BRAIN; CELL-LINES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
49
Recensione:
Indirizzi per estratti:
Indirizzo: Beach, JW UnivAGeorgia, Coll Pharm, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 US Univ Georgia Athens GA USA 30602 iomed Sci, Athens, GA 30602 US
Citazione:
J.W. Beach et al., "Synthesis and in vivo and in vitro evaluation isoarecolone and derivatives", MED CHEM RE, 8(9), 1998, pp. 510-522

Abstract

The synthesis of the N-ethyl and N-phenylethyl derivatives of isoarecoloneare described. These compounds were evaluated in vitro for their ability to displace [H-3](+/-)epibatidine and/or [H-3](-) nicotine from nicotinic receptors derived from rat cerebral cortex and their ability to inhibit acetylcholinesterase. The N-ethyl derivative and isoarecolone were evaluated in vivo for their antinociceptive, hypothermia and hypomotility activity in mice. The in vivo activity of isoarecolone was found to the reversible by mecamylamine, however the N-ethyl derivative was found to be insensitive to blockade by mecamylamine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/09/20 alle ore 22:00:51