CMPI hydrochloride, a potent and selective nAChR agonist, functions as a positive allosteric modulator (PAM) specifically targeting the α4:α4 subunit interface of the nAChR. It enhances the response of the (α4)3(β2)2 nAChR to acetylcholine (ACh) (10 μM) with an EC 50 of 0.26 μM. With its potential for researching nicotine dependence and various neuropsychiatric conditions linked to reduced brain cholinergic activity, CMPI hydrochloride stands as a significant compound in neurological research.

CMPI (0.01-10 μM) potentiates (α4) 3 (β2) 2 (low ACh sensitivity) but not (α4) 2 (β2) 3 (high ACh sensitivity) nAChRs in Xenopus laevis oocytes[1]. CMPI (0.01-10 μM) inhibits (α4) 2 (β2) 3 , human muscle and Torpedo nAChRs with IC 50 s of 0.6, 0.7 and 0.2 μM, respectively in Xenopus oocytes[1].