Trimeprazine (tartrate)

Trimeprazine is a histamine H1 receptor antagonist (Ki = 0.72 nM in a radioligand binding assay). It is selective for the histamine H1 receptor over muscarinic acetylcholine receptors (mAChRs, Ki = 38 nM in a radioligand binding assay). Trimeprazine inhibits anti-IgE-induced histamine release from isolated human lung fragments (IC50 = 19 nM) but induces histamine release with a 50% release concentration (RC50) of 1.03 µM. It reduces severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.76 µM) with a 50% cytotoxic concentration (CC50) value of 19.73 µM. Formulations containing trimeprazine have been used in the treatment of allergic pruritis and motion sickness.Formal Name: N,N,beta-trimethyl-10H-phenothiazine-10-propanamine, 2R,3R-dihydroxybutanedioate. CAS Number: 4330-99-8. Synonyms: Alimemazine, NSC 17475. Molecular Formula: C18H22N2S . 1/2C4H6O6. Formula Weight: 373.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml, PBS (pH 7.2): insol. lambdamax: 252 nm. SMILES: CN(C)CC(C)CN1C2=CC=CC=C2SC3=CC=CC=C31.OC([C@H](O)[C@@H](O)C(O)=O)=O. InChi Code: InChI=1S/2C18H22N2S.C4H6O6/c2*1-14(12-19(2)3)13-20-15-8-4-6-10-17(15)21-18-11-7-5-9-16(18)20,5-1(3(7)8)2(6)4(9)10/h2*4-11,14H,12-13H2,1-3H3,1-2,5-6H,(H,7,8)(H,9,10)/t,,1-,2-/m..1/s1. InChi Key: AJZJIYUOOJLBAU-CEAXSRTFSA-N.