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].

nAChR^[1]

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 IC₅₀s of 0.6, 0.7 and 0.2 µM, respectively in Xenopus oocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

379.28

C₁₈H₂₀Cl₂N₄O

2250025-94-4

CC1=C(C2=CC(C3=CC=CC=C3Cl)=NO2)C=NN1C4CCNCC4.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]