Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonists.

ABSTRACT: Partial agonist therapies rely variously on two hypotheses: the partial agonists have their effects through chronic low-level receptor activation or the partial agonists work by decreasing the effects of endogenous or exogenous full agonists. The relative significance of these activities probably depends on whether acute or chronic effects are considered. We studied nicotinic acetylcholine receptors (nAChRs) expressed in Xenopus laevis oocytes to test a model for the acute interactions between acetylcholine (ACh) and weak partial agonists. Data were best-fit to a basic competition model that included an additional factor for noncompetitive inhibition. Partial agonist effects were compared with the nAChR antagonist bupropion in prolonged bath application experiments that were designed to mi

SUBMITTER: Papke RL 

PROVIDER: S-EPMC3083103 | biostudies-literature | 2011 May

REPOSITORIES: biostudies-literature