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Titolo:
Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist
Autore:
Damaj, MI; Glassco, W; Aceto, MD; Martin, BR;
Indirizzi:
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 PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
fascicolo: 1, volume: 291, anno: 1999,
pagine: 390 - 398
SICI:
0022-3565(199910)291:1<390:AAPEOM>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
CNS SELECTIVITY; SPINAL-CORD; MICE; RAT; ACETYLCHOLINE; EPIBATIDINE; MODEL; PAIN; ENANTIOMERS; RJR-2403;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
34
Recensione:
Indirizzi per estratti:
Indirizzo: Damaj, MI Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol & Toxicol, Box 980613, Richmond, VA 23298 USA Virginia Commonwealth Univ Box 980613 Richmond VA USA 23298 USA
Citazione:
M.I. Damaj et al., "Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist", J PHARM EXP, 291(1), 1999, pp. 390-398

Abstract

Metanicotine [N-methyl-4-(3-pyridinyl)-3-butene-1-amine], a novel neuronalnicotinic agonist, was found to bind with high affinity (K-i = 24 nM) to rat brain [H-3] nicotine binding sites and it generalized to nicotine in a dose-dependent manner in the drug discrimination procedure. Metanicotine produced significant antinociceptive effects in mice and rats subjected to either acute thermal (tail-flick), mechanical (paw-pressure), chemical (para-phenylquinone), persistent (Formalin), and chronic (arthritis) pain stimuli. Metanicotine was about 5-fold less potent than nicotine in the tail-flick test after s.c administration, but slightly more potent after central administration. Its duration of action was longer than that of nicotine. Nicotinic antagonists, mecamylamine and dihydro-beta-erythroidine, blocked metanicotine-induced antinociception in the different pain models. However, the antinociceptive effect was not affected by pretreatment with either naloxone or by atropine, confirming that metanicotine exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms. In contrast to nicotine, antinociceptive effects of metanicotine were observed at doses that had virtually no effect on spontaneous activity and body temperature in mice. These data indicate that metanicotine is a centrally actingneuronal nicotinic agonist with preferential antinociceptive effects in animals. Thus, metanicotine and related nicotinic agonists may have great potential for development as a new class of analgesics.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/09/20 alle ore 07:30:45