Buy Mepyramine (pyrilamine) Cas 91-84-9

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Buy Mepyramine (pyrilamine) Cas 91-84-9

Mepyramine, also known as pyrilamine, is a first-generation antihistamine, targeting the H1 receptor as an inverse agonist.[1] Mepyramine rapidly permeates the brain, often causing drowsiness.[2] It is often sold as a maleate salt, pyrilamine maleate.

The medication has negligible anticholinergic activity, with 130,000-fold selectivity for the histamine H1 receptor over the muscarinic acetylcholine receptors (for comparison, diphenhydramine had 20-fold selectivity for the H1 receptor).[3]

It was patented in 1943 and came into medical use in 1949.[4] It was marketed under the names Histadyl, Histalon, Neo-Antergan, Neo-Pyramine, and Nisaval.[5] In the 1960s and 70s it was a very common component in over-the-counter sleep aids such as Alva-Tranquil, Dormin, Sedacaps, Sominex, Nytol, and many others.[5] The US Food and Drug Administration (FDA) included it in the list of chemicals and compounds barred from use in over-the-counter (OTC) nighttime sleep aid products in 1989.[6]

It is used in over-the-counter combination products to treat the common cold and menstrual symptoms such as Midol Complete.[7] It is also the active ingredient of the topical antihistamine creams Anthisan[8] and Neoantergan[1] sold for the treatment of insect bites, stings, and nettle rash.

See also

References

  1.  Parsons ME, Ganellin CR (January 2006). “Histamine and its receptors”British Journal of Pharmacology147 (Suppl 1) (published 2 February 2009): S127–S135. doi:10.1038/sj.bjp.0706440PMC 1760721PMID 16402096.
  2.  “Mepyramine”drugbank.com. Retrieved 8 May 2021.
  3.  Kubo N, Shirakawa O, Kuno T, Tanaka C (March 1987). “Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay”Japanese Journal of Pharmacology43 (3): 277–282. doi:10.1254/jjp.43.277PMID 2884340.
  4.  Fischer J, Gannelin CR, eds. (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 545. ISBN 9783527607495.
  5.  Thornton WE (September 1977). “Sleep aids and sedatives”. Journal of the American College of Emergency Physicians6 (9): 408–412. doi:10.1016/S0361-1124(77)80006-3PMID 330911.
  6.  54 FR 6826
  7.  “Active Ingredients for Midol Complete”Bayer HealthCare LLC. Archived from the original on 2 December 2009. Retrieved 8 December 2009.
  8.  “Anthisan Cream – Patient Information Leaflet (PIL)”Medicines.org.

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