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- W2066012977 abstract "Nornicotine, a major tobacco alkaloid and nicotine metabolite, accumulates in rat brain in pharmacologically relevant concentrations following repeated nicotine administration. Nornicotine-evoked striatal dopamine release is Ca2+-dependent, stereoselective and sensitive to nicotinic receptor antagonists, indicating nicotinic receptor-mediation. The present study determined if S-(−)-nornicotine desensitizes nicotinic receptors and if cross-desensitization to S-(−)-nicotine occurs. S-(−)-Nicotine (10 and 100 nM) diminished [3H]overflow from [3H]dopamine-preloaded rat striatal slices following subsequent superfusion with 10 μM S-(−)-nicotine (46% and 74%, respectively) or 10 μM S-(−)-nornicotine (59% and 81%, respectively). S-(−)-Nornicotine (1 and 10 μM) diminished the response to subsequent superfusion with 10 μM S-(−)-nornicotine (85% and 97%, respectively) or 10 μM S-(−)-nicotine (82% and 88%, respectively). Thus, similar to S-(−)-nicotine, S-(−)-nornicotine desensitizes nicotinic receptors, but with ∼12-fold lower potency. Cross-desensitization suggests involvement of common nicotinic receptor subtypes. Therefore, S-(−)-nicotine metabolites, such as nornicotine, have neuropharmacologically relevant effects." @default.
- W2066012977 created "2016-06-24" @default.
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- W2066012977 date "2001-09-01" @default.
- W2066012977 modified "2023-09-26" @default.
- W2066012977 title "Nornicotine, a nicotine metabolite and tobacco alkaloid: desensitization of nicotinic receptor-stimulated dopamine release from rat striatum" @default.
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- W2066012977 doi "https://doi.org/10.1016/s0014-2999(01)01283-3" @default.
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