Mepyramine, also known as pyrilamine, is a first generation antihistamine, targeting the H1 receptor. 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. It is used in over-the-counter combination products to treat the common cold and menstrual symptoms. 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.
- ↑ Parsons, Mike E.; Ganellin, C. Robin (January 2006). "Histamine and its receptors". British Journal of Pharmacology. 147 (S1): S127–S135. 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): 277–282. ISSN 0021-5198. PMID 2884340.
- ↑ Active Ingredients for Midol Complete
- ↑ R.J. Horclois, U.S. Patent 2,502,151 (1950), to Rhône-Poulenc.
- ↑ Huttrer, C. P.; Djerassi, C.; Beears, W. L.; Mayer, R. L.; Scholz, C. R. (1946). "Heterocyclic amines with antithistaminic activity". Journal of the American Chemical Society. 68 (10): 1999–2002. doi:10.1021/ja01214a037. PMID 21001124.
- ↑ D. Bovet, R. Horclois, F. Walthert, C.R. Soc. Biol., 138, 99 (1944).