Abstract
Nicotinic acetylcholine receptors (nAChRs) belong to the superfamily of ligand-gated ion channels. The most abundant homomeric nAChR in the mammalian brain are the pentameric α7 nAChRs, which consist of five α7 subunits. Positive allosteric modulators (PAMs) of nAChRs have been implicated to be putative therapeutics in the pharmacological treatment of Alzheimer's disease, schizophrenia and Parkinson's disease.Recently, Sitzia et al. (2011) showed a striking temperature dependence for positive allosteric modulation of PNU-120596 on nAChRs. The aim of our study was to investigate the temperature dependence of other PAMs on nACHRs with automated patch clamp techniques. For this study, we have used GH4C1cells expressing human nAChR α7 subunits. Electrophysiological recordings were performed on the Patchliner, a robotic patch clamp device allowing temperature controlled recordings from up to 8 cells simultaneously.View Large Image | View Hi-Res Image | Download PowerPoint SlideFirst experiments on GABA A receptors allude to a similar but weaker effect on the temperature dependence of PAMs.These data suggest that experiments on the efficacy of PAMs conducted at room temperature have to be interpreted with caution.Sitzia et al (2011) FrontPharmacol;2:81.
Published Version
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