Mepyramine
Mepyramine, also known as pyrilamine, is a first generation antihistamine, targeting the H1 receptor as an inverse agonist.[1] It rapidly permeates the brain often causing drowsiness. It also has anticholinergic properties. However, its anticholinergic potency is negligible compared to its antihistaminergic activity; it has an H1 to muscarinic Ki ratio of 130,000 to 1, compared to a ratio of 20 to 1 for diphenhydramine.[2]
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| Other names | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine |
| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a606008 |
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| ECHA InfoCard | 100.001.912  |
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| Formula | C17H23N3O |
| Molar mass | 285.391 g·mol−1 |
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It was patented in 1943 and came into medical use in 1949.[3] It is used in over-the-counter combination products to treat the common cold and menstrual symptoms.[4] It is also the active ingredient of the topical antihistamine creams Anthisan and Neoantergan sold for the treatment of insect bites, stings, and nettle rash.
See also
- Chloropyramine (chloro instead of methoxy)
References
- Parsons ME, Ganellin CR (January 2006). "Histamine and its receptors". British Journal of Pharmacology. 147 Suppl 1 (S1): S127-35. doi:10.1038/sj.bjp.0706440. PMC 1760721. PMID 16402096.
- Kubo N, Shirakawa O, Kuno T, Tanaka C (March 1987). "Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay". Japanese Journal of Pharmacology. 43 (3): 277–82. doi:10.1254/jjp.43.277. PMID 2884340.
- Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 545. ISBN 9783527607495.
- "Active Ingredients for Midol Complete". Archived from the original on 2009-12-02. Retrieved 2009-12-08.
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Antihistamines (R06) | |
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