2250025-94-4

2250025-94-4 structure

Name: nAChR agonist CMPI hydrochloride
Chemical Name: nAChR agonist CMPI hydrochloride
CAS Number: 2250025-94-4
Molecular Formula: C₁₈H₂₀Cl₂N₄O
Molecular Weight: 379.28
Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
Create Date: 2020-12-03 18:52:58
Modify Date: 2024-01-10 19:33:17
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].

Name	nAChR agonist CMPI hydrochloride

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR Signaling Pathways >> Neuronal Signaling >> nAChR Research Areas >> Neurological Disease
Target	nAChR[1]
In Vitro	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].
References	[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. [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.

Molecular Formula	C₁₈H₂₀Cl₂N₄O
Molecular Weight	379.28