pyrilamine

Also known as Anthisan®, mepiramine, mepyramine maleate, pyrilamine tannate, Pyrlex®, N',N'-dimethyl-N-(p-methoxybenzyl)-N-(2-pyridyl)ethylenediamine, N-(p-methoxybenzyl)-N',N'-dimethyl-N-(alpha-pyridyl)ethylenediamine

Mepyramine, also known as pyrilamine, is a first-generation antihistamine, targeting the H1 receptor as an inverse agonist. Mepyramine rapidly permeates the brain, often causing drowsiness.

Research

2,541 papers

Physical and biological properties of pyrilamine.Journal of pharmaceutical sciences · 1983
[Research progress of pyrilamine-sensitive H~+/OC antiporter].Yao xue xue bao = Acta pharmaceutica Sinica · 2016
Pyrilamine-sensitive proton-coupled organic cation (H(+)/OC) antiporter for brain-specific drug delivery.Journal of controlled release : official journal of the Controlled Release Society · 2017
Involvement of proton-coupled SLC49A4-mediated transport in the export of lysosomally trapped pyrilamine.Drug metabolism and disposition: the biological fate of chemicals · 2023
Chronic feeding study of pyrilamine in Fischer 344 rats.Fundamental and applied toxicology : official journal of the Society of Toxicology · 1995

via PubMed

Wikidata facts

Mass: 285.184112

Show 3 more facts

chemical formula: C₁₇H₂₃N₃O
canonical SMILES: CN(C)CCN(CC1=CC=C(C=C1)OC)C2=CC=CC=N2
Commons category: Mepyramine

Sources (3)

via Wikidata · CC0

~2 min read

Article

2 sections

Contents

See also
References

Mepyramine, also known as pyrilamine, is a first-generation antihistamine, targeting the H1 receptor as an inverse agonist. Mepyramine rapidly permeates the brain, often causing drowsiness. 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).