Formulation: A solid
Formal Name: N,N,β-trimethyl-10H-phenothiazine-10-propanamine, 2R,3R-dihydroxybutanedioate
Purity: ≥98%
Formula Markup: C18H22N2S • 1/2C4H6O6
Formula Weight: 373,5
Shelf life (days): 1460
CAS Number: 4330-99-8
Notes: Trimeprazine is a histamine H1 receptor antagonist (Ki = 0.72 nM in a radioligand binding assay).{23214} 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.{52786} 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.{62432} Formulations containing trimeprazine have been used in the treatment of allergic pruritis and motion sickness.
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