(S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems[1].
in vivo
PNU-282987 (free base) (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit[1].
PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner[1].
References
[1] Bodnar AL, Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8. DOI:10.1021/jm049363q