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nAChR agonist CMPI hydrochloride

Names

[ CAS No. ]:
2250025-94-4

[ Name ]:
nAChR agonist CMPI hydrochloride

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H20Cl2N4O

[ Molecular Weight ]:
379.28

Related Compounds