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Titolo:
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2 '-substituted-3 ' phenyl-5 '-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel nicotinic antagonist
Autore:
Carroll, FI; Lee, JR; Navarro, HA; Brieaddy, LE; Abraham, P; Damaj, MI; Martin, BR;
Indirizzi:
Res Triangle Inst, Res Triangle Pk, NC 27709 USA Res Triangle Inst Res Triangle Pk NC USA 27709 Triangle Pk, NC 27709 USA Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA Virginia Commonwealth Univ Richmond VA USA 23298 , Richmond, VA 23298 USA
Titolo Testata:
JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 24, volume: 44, anno: 2001,
pagine: 4039 - 4041
SICI:
0022-2623(20011122)44:24<4039:SNARBA>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
MICE;
Tipo documento:
Letter
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
11
Recensione:
Indirizzi per estratti:
Indirizzo: Carroll, FI Res Triangle Inst, POB 12194, Res Triangle Pk, NC 27709 USA Res Triangle Inst POB 12194 Res Triangle Pk NC USA 27709 9 USA
Citazione:
F.I. Carroll et al., "Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2 '-substituted-3 ' phenyl-5 '-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel nicotinic antagonist", J MED CHEM, 44(24), 2001, pp. 4039-4041

Abstract

A series of 2'-substituted-3'-phenyl epibatidine analogues were synthesized and evaluated for inhibition of binding at nicotine acetylcholine receptors and for antinociceptive properties in mice. The introduction of a bulky phenyl group at the T-position exerted a profound influence on both receptor binding and antinociceptive effects. Substitution of different groups at the 2'-position distinguished between agonist and antagonist properties. These results demonstrate that structural requirements for receptor activities and recognition are distinctively different.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/09/20 alle ore 21:25:14