Title : Nicotinic receptor antagonists as treatments for nicotine abuse.

Pub. Date : 2014

PMID : 24484986






2 Functional Relationships(s)
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1 Receptor antagonists that selectivity target central nAChR subtypes mediating nicotine-evoked DA release should have efficacy as tobacco use cessation agents with the therapeutic advantage of a limited side-effect profile. Nicotine cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus
2 More recent data have shown that novel, nonquaternary bis-1,2,5,6-tetrahydropyridine analogs potently inhibit (IC50<1nM) nicotine-evoked DA release in vitro by acting as antagonists at alpha-CtxMII-sensitive nAChR subtypes; these compounds also decrease NIC self-administration in rats. Nicotine cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus