pnu282987-hcl

Description: PNU-282987 is a novel, potent and selective agonist of alpha7 nicotinic acetylcholine receptor(alpha7 nAChR) with Ki of 26 nM; it has no affinity for alpha1beta1gammadelta and alpha3beta4 nAChRs (IC50 >= 60 uM). In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282, 987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget. PNU-282987 evoked whole-cell currents from cultured rat hippocampal neurons that were sensitive to the selective alpha7 nAChR antagonist methyllycaconitine (MLA) and enhanced GABAergic synaptic activity when applied to hippocampal slices.

References: J Pharmacol Exp Ther. 2005 Mar; 312(3):1213-22.

Related CAS#:123464-89-1 (free base); 737727-12-7 (S-enantiomer of PNU-282987 free base)