Thiazinamium chloride 

Thiazinamium (chloride) possesses potent anticholinergic and antiallergic activity and inhibits TxB2 synthesis with IC₅₀ value of 0.2 µM. Thiazinamium (chloride) is structurally similar to H-1 antagonists Promethazine (HY-B1296). Thiazinamium (chloride) stimulates the phosphatidylcholine secretion in adult rat type II pneumocytes^[1][2].

IC50: 0.2 µM (TxB2 synthesis)^[1]

TxB2 synthesis by resting macrophages is inhibited by thiazinamium chloride and promethazine in a dose-dependent manner. Thiazinamium chloride inhibits TxBz synthesis but had no effect on the ingestion of zymosan particles. In contrast, chlorpromazine inhibits phagocytosis but not TxBz synthesis except at lo^-3 M. Under the condition where indomethacin, a nown cyclooxygenase inhibitor, is inhibitory, promethazine but not thiazinamium chloride inhibits TxB2 synthesis from exogenous arachidonic acid. Treatment of macrophages with promethazine and chlorpromazine but not thiazinamium chloride results in a reduction in the oxidative burst during phagocytosis. Furthermore, the ability of thiazinamium chloride to selectively inhibit arachidonic acid metabolism may contribute to its bronchodilator/antiallergic activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

334.91

C₁₈H₂₃ClN₂S

4320-13-2

Solid

White to off-white

C[N+](C)(C)C(C)CN1C2=C(C=CC=C2)SC3=CC=CC=C13.[Cl-]

Room temperature in continental US; may vary elsewhere.

• [1]. Chang J, et al. Effects of thiazinamium chloride, promethazine and chlorpromazine on thromboxane B2 synthesis, phagocytosis and respiratory burst by rat alveolar macrophages. Biochem Pharmacol. 1983 Sep 15;32(18):2671-7.  [Content Brief]

  [2]. Gilfillan, A. M., et al., (1987). Effects of thiazinamium chloride and other antihistamines on phosphatidylcholine secretion in rat type II pneumocyte cultures. Biochemical pharmacology, 36(2), 277–281.