Mepyramine maleate CAS: 59-33-6
MF: C21H27N3O5
MW: 401.46
A histamine H1 receptor antagonist.

Mepyramine maleate (CAS 59-33-6)

Mepyramine maleate | CAS 59-33-6 is rated 5.0 out of 5 by 1.
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Application: A histamine H1 receptor antagonist
CAS Number: 59-33-6
Molecular Weight: 401.46
Molecular Formula: C21H27N3O5
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Mepyramine maleate is a histamine H1 receptor antagonist and binds with high affinity to G(q/11) protein. Mepyramine maleate is found to be a potent inhibitor of CYP2D6 (P450 2D forms) in hepatocytes, and PAF-induced platelet aggregation. Mepyramine maleate is commonly utilized as a radioligand ([3H]Mepyramine) binding assay for the H1 receptor. This product has been recently discovered to exhibit blocking ability of KCNQ/M channels which is potentially related to an adverse effect seen in excess intake of antihistamines.


References

1. Liu, Y.Q., et al. 1992. Biochem. Biophys. Res. Commun. 189: 378-384. PMID: 1449491
2. Zeng, S. and Guo, Z.G. 1997. Zhongguo Yao Li Xue Bao. 18: 155-158. PMID: 10072970
3. Vleeming, W., et al. 2000. Br. J. Pharmacol. 129: 1801-1807. PMID: 10780989
4. Fitzsimons, C.P., et al. 2004. J. Biol. Chem. 279: 34431-34439. PMID: 15192105
5. Liu, B., et al. 2008. Neuropharmacology. 54: 629-639. PMID: 18222495

Appearance :
Crystalline powder
Physical State :
Solid
Solubility :
Soluble in water (100 mg/ml), methanol, Phosphate buffered saline (100 mM), alcohol (1: 2.5 - 3.0), and chloroform (1: 2).
Storage :
Store at room temperature
Melting Point :
98.9-102.8° C
Boiling Point :
423.8° C at 760 mmHg (Predicted)
Refractive Index :
n20D 1.58 (Predicted)
IC50 :
Adenosine A3-R: IC50 = 1.3 nM (human); Histamine H1 Receptor: IC50 = 1.5 nM (human); Histamine H1 receptor: IC50 = 34 nM (Cavia porcellus); ST: IC50 = 47 nM (human); CYP2D6: IC50 = 0.3 µM (human)
Ki Data :
Histamine H1 Receptor: Ki= 0.43 nM (human); ST: Ki= 25 nM (human); SR-2A: Ki= 285 nM (human); SR-2C: Ki= 592 nM (human); σReceptor: Ki= 655 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UT1225000
PubChem CID :
5284451
Merck Index :
14: 7984
MDL Number :
MFCD00069333
EC Number :
200-422-7
SMILES :
CN(C)CCN(CC1=CC=C(C=C1)OC)C2=CC=CC=N2.C(=C\\C(=O)O)\\C(=O)O

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Mepyramine maleate  Product Citations

See how others have used Mepyramine maleate. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 28912446  Hong, LTA. et al. 2017. Nat Commun. 8: 533.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Liu Liu, B. et al. (PubMed 18222495) reported that the antihistamine Mepyramine maleate directly inhibits KCNQ/M channel and depolarizes rat superior cervical ganglion neurons. -SCBT Publication Review
Date published: 2015-06-08
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