Tripelennamine (hydrochloride)

Tripelennamine is a histamine H1 receptor antagonist (Ki = 7. nM). It is selective for the histamine H1 receptor over muscarinic acetylcholine receptors (mAChRs, Ki = 1,300 nM). Tripelennamine also selectively inhibits histamine- over acetylcholine-induced contractions in isolated guinea pig ileum segments (EC50s = 14 and 7,800 nM, respectively), as well as serotonin-induced contractions in isolated rat uterus (EC50 = 14,000 nM). It protects against histamine-induced lethality and dyspnea in guinea pigs with half-maximal protective dose (PD50) values of 2. and 1. mg/kg, respectively. Formulations containing tripelennamine have been used as antihistamines in veterinary medicine. InChI: InChI=1S/C16H21N3.ClH/c1-18(2)12-13-19(16-10-6-7-11-17-16)14-15-8-4-3-5-9-15,/h3-11H,12-14H2,1-2H3,1H InChIKey: FSSICIQKZGUEAE-UHFFFAOYSA-N SMILES: CN(C)CCN(CC1=CC=CC=C1)C2=NC=CC=C2.Cl