Synonyms
10-(3-(dimethylamino)propyl)-phenothiazinmonohydrochloride;10-(gamma-Dimethylamino-n-propyl)phenothiazine hydrochloride
Molecular Formula
C17H21ClN2S
Smiles
CN(C)CCCN1C2=CC=CC=C2SC3=CC=CC=C31.Cl
General Description
Promazine Hydrochloride is a phenothiazine-derived compound belonging to the aliphatic phenothiazine subclass. It is one of the earliest phenothiazine compounds developed for clinical use, possessing a tricyclic ring system with a dimethylaminopropyl side chain at the N-10 position.
Mechanism of Action
Promazine Hydrochloride acts primarily as a dopamine D2 receptor antagonist in the mesolimbic and mesocortical pathways, with additional antagonist activity at histamine H1, muscarinic cholinergic, and alpha-1 adrenergic receptors. Its multi-receptor profile underlies both its antipsychotic efficacy and associated pharmacological effects.
Application
Used in the treatment of psychotic disorders including schizophrenia and severe anxiety states. Promazine Hydrochloride is an aliphatic phenothiazine antipsychotic that acts primarily as a dopamine D2 receptor antagonist. It is also used in the management of nausea, intractable hiccups, and as an adjunct in tetanus treatment.
Promazine hydrochloride was identified as a selective inhibitor of the MALT1 paracaspase protease in activated B cell-like diffuse large B cell lymphoma (ABC-DBLC).
The mechanism of action involved noncompetitive inhibition of MALT1 proteolytic activity, which was demonstrated through both recombinant enzyme assays and cellular systems. By blocking MALT1 cleavage activity, promazine effectively inhibited downstream anti-apoptotic NF-κB signaling, a pathway essential for the survival of ABC-DLBCL cells. This selective pathway inhibition resulted in potent cytotoxic effects exclusively on MALT1-dependent lymphoma cells both in vitro and in vivo, while sparing MALT1-independent cell types. The study provided conceptual proof that distinct phenothiazine derivatives, including promazine, could be repurposed for the targeted treatment of aggressive ABC-DLBCL through this previously unrecognized mechanism of MALT1 protease inhibition.
Fig. 1 PD Treatment Impairs MALT1 Activity in ABC-DLBCL Cells. (Nagel D.; et al. 2012)
References
- Nagel D, et al. Pharmacologic inhibition of MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL. Cancer cell, 2012, 22(6): 825-837.
How does Promazine Hydrochloride compare to chlorpromazine in clinical efficacy?
Promazine Hydrochloride has lower potency at dopamine D2 receptors compared to chlorpromazine, resulting in a different side-effect profile that may be preferable for certain patient populations.
What storage conditions are required for Promazine Hydrochloride?
Promazine Hydrochloride should be stored at 2-8℃ in a tightly sealed container, protected from light and moisture.
What purity grade is available for Promazine Hydrochloride?
Promazine Hydrochloride is supplied as a high-purity grade suitable for R&D and pharmaceutical manufacturing.
Can order specifications and packaging be customized?
Yes, packaging can be customized for various order sizes, from small laboratory quantities to bulk production shipments.