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Titolo:
PHARMACOLOGY OF LOBELINE, A NICOTINIC RECEPTOR-LIGAND
Autore:
DAMAJ MI; PATRICK GS; CREASY KR; MARTIN BR;
Indirizzi:
VIRGINIA COMMONWEALTH UNIV,MED COLL VIRGINIA,DEPT PHARMACOL & TOXICOLRICHMOND VA 23298
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 282, anno: 1997,
pagine: 410 - 419
SICI:
0022-3565(1997)282:1<410:POLANR>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN MEMBRANES; CONDITIONED TOLERANCE; MOUSE-BRAIN; BINDING; AGONISTS; ACETYLCHOLINE; (-)-NICOTINE; MORPHINE; SITES; MICE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
M.I. Damaj et al., "PHARMACOLOGY OF LOBELINE, A NICOTINIC RECEPTOR-LIGAND", The Journal of pharmacology and experimental therapeutics, 282(1), 1997, pp. 410-419

Abstract

In this study we investigated the pharmacology of lobeline, a high affinity nicotinic ligand with a unique pharmacological profile, in different in vitro and in vivo tests. Although lobeline displaced [H-3]-nicotine binding sites in the rat brain with a K-I of 4.4 nM, it did notactivate alpha 4 beta 2 expressed receptors in frog oocytes. The in vivo pharmacological effects of lobeline were highly complex. Lobeline,at the time of maximal effect, dose-dependently produced motor impairment and decreased locomotor activity and body temperature in mice after s.c. treatment. However, antinociception was present after intrathecal but not after s.c. administration of lobeline in the tail-flick tests. The behavioral effects of lobeline were not blocked by pretreatment with either mecamylamine or dihydro-beta-erythroidine. in addition,lobeline given s.c. enhanced nicotine-induced antinociception in a dose-related manner. No acute tolerance developed to either lobeline's behavioral or antinociceptive effect after s.c. or intrathecal administration, respectively. However, tolerance developed to lobeline's pharmacological effects after chronic treatment with the drug for 10 days (15 mg/kg, s.c. twice a day). Furthermore, cross-tolerance between lobeline and nicotine developed after chronic treatment with either drug. Although the alpha 4 beta 2 receptor is unlikely to mediate the agonist effects of lobeline, our results indicate that lobeline does interact with the nicotinic receptor in a novel fashion.

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