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Titolo:
Chain-lengthened and imidazoline analogues of nicotine
Autore:
Ferretti, G; Dukat, M; Giannella, M; Piergentili, A; Pigini, M; Quaglia, W; Damaj, MI; Martin, BR; Glennon, RA;
Indirizzi:
Virginia Commonwealth Univ, Sch Pharm, Dept Med Chem, Richmond, VA 23298 USA Virginia Commonwealth Univ Richmond VA USA 23298 , Richmond, VA 23298 USA Univ Camerino, Dipartimento Sci Chim, I-6032 Camerino, Italy Univ Camerino Camerino Italy I-6032 nto Sci Chim, I-6032 Camerino, Italy Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA Virginia Commonwealth Univ Richmond VA USA 23298 , Richmond, VA 23298 USA
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 23, volume: 10, anno: 2000,
pagine: 2665 - 2668
SICI:
0960-894X(200012)10:23<2665:CAIAON>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACETYLCHOLINE-RECEPTOR LIGANDS; MICE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
11
Recensione:
Indirizzi per estratti:
Indirizzo: Giannella, M Virginia Commonwealth Univ, Sch Pharm, Dept Med Chem, Richmond, VA 23298 USA Virginia Commonwealth Univ Richmond VA USA 23298 A 23298 USA
Citazione:
G. Ferretti et al., "Chain-lengthened and imidazoline analogues of nicotine", BIOORG MED, 10(23), 2000, pp. 2665-2668

Abstract

Analogues of nicotine (1) and azanicotine (3) were prepared with an additional methylene group inserted between the two rings (i.e., homonicotine andhomoazanicotine; 6 and 5, respectively). Although 6 (K-i = 3110 nM) and 3 (K-i = 206 nM) bind at nACh receptors with greater than or equal to 100-fold lower affinity than nicotine (K-i=2.1nM), 5 displays high affinity (K-i=7.8nM). Like nicotine (ED50=12 mug/mouse), both 3 and 5 (ED50=21 and 19 mug/mouse, respectively) produced antinociceptive activity in the tail-flick assay following intrathecal administration. The antinociceptive actions of 3 and 5, unlike those of nicotine, were not antagonized by mecamylamine. Compounds 3 and 5 might represent novel analgesic agents that act via a non-nicotinic mechanism, or via a nicotinic mechanism that is distinct from that mediating the antinociceptive actions of nicotine. (C) 2000 Elsevier ScienceLtd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/09/20 alle ore 16:13:49