nAChR agonist CMPI hydrochloride

Modify Date: 2024-01-10 19:33:17

nAChR agonist CMPI hydrochloride Structure
nAChR agonist CMPI hydrochloride structure
Common Name nAChR agonist CMPI hydrochloride
CAS Number 2250025-94-4 Molecular Weight 379.28
Density N/A Boiling Point N/A
Molecular Formula C18H20Cl2N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name nAChR agonist CMPI hydrochloride

 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
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
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