nAChR agonist CMPI hydrochloride

nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 μM) with an EC50 of 0.26 μM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity[1][2].

CMPI hydrochloride is a potent positive allosteric modulator of α4β2 nAChRs (EC50 values are 20 and 18 nM for rat and human, respectively). Selective for hα4β2 over hα3β2, hα3β4 and hα7. Inhibits (α4)2(β2)3, muscle-type and Torpedo nAChRs (IC50 values are 0.5, 0.7 and 0.2 μM, respectively), but not (α4)3(β2)2 receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains.

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[1] Hamouda AK, et, al. Photolabeling a Nicotinic Acetylcholine Receptor (nAChR) with an (α4)3(β2)2 nAChR-Selective Positive Allosteric Modulator. Mol Pharmacol. 2016 May;89(5):575-84. DOI:10.1124/mol.116.103341
[2] Wang ZJ, et, al. Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses. J Biol Chem. 2017 Jun 16;292(24):9988-10001. DOI:10.1074/jbc.M116.771246