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.
For research use only. We do not sell to patients.
- CAS No.: 2250025-94-4
- Formula: C18H20Cl2N4O
- Molecular Weight:379.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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CAS No. 2250025-94-4
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Molecular Weight 379.28
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Formula C18H20Cl2N4O
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SMILES
CC1=C(C2=CC(C3=CC=CC=C3Cl)=NO2)C=NN1C4CCNCC4.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
nAChR agonist CMPI hydrochloride Related Classifications
HY-136258 Related Classifications
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