Cayman Trimeprazine (tartrate)

Trimeprazine is a histamine H₁ receptor antagonist (K_i = 0.72 nM in a radioligand binding assay).¹ It is selective for the histamine H₁ receptor over muscarinic acetylcholine receptors (mAChRs; K_i = 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.² 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.³ Formulations containing trimeprazine have been used in the treatment of allergic pruritis and motion sickness.

WARNING This product is not for human or veterinary use.