Progress in understanding the CNS nicotinic acetylcholine receptor (nAChR) has been hindered by the absence of an antagonist that both biochemically binds receptor sites and blocks physiological activity. In contrast with the mammalian muscle nAChR, there is an apparent dissociation between the in vitro and in vivo behavior of CNS cholinergic antagonists. The biochemistry, pharmacology and physiology of brain nAChRs are discussed here. It is suggested that some of the discrepancies among these approaches can be reconciled by proposing multiple binding sites for cholinergic agents.
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