Propionylpromazine (hydrochloride)

Propionylpromazine is a promazine neuroleptic and dopamine receptor antagonist.^1,2,3 It is an antagonist at the I. scapularis (tick) dopamine 2 receptor (Isdop2) and A. aegypti (mosquito) dopamine 2 receptor (AaDOP2), providing 94 and 85% inhibition, respectively, in a chemical screening assay at 10 µM.^4,3 Propionylpromazine inhibits recombinant T. cruzi trypanothione reductase (IC₅₀ = 357 µM) and is active against T. brucei trypomastigotes (ED50 = 10.1 µM) but not L. donovani amastigotes or T. cruzi trypomastigotes (ED₅₀s = >30 µM) in mouse peritoneal macrophages.⁵ It increases survival of C. elegans in a model of paraquat-induced oxidative stress.⁶ Propionylpromazine reduces stereotypic behavior induced by apomorphine in rats (ED₅₀ = 2.5 mg/kg, s.c.).¹ Formulations containing propionylpromazine have been used as tranquilizers in veterinary medicine.

WARNING This product is not for human or veterinary use.

1. Fielding, S., and Lal, H. Biochemical actions of neuroleptic drugs: focus on the dopamine receptor. Handbook of psychopharmacology 37-55 (1978).

2. Ejendal, K.F.K., Meyer, J.M., Brust, T.F., et al. Discovery of antagonists of tick dopamine receptors via chemical library screening and comparative pharmacological analyses. Insect Biochem. Molec. 42(11), 846-853 (2012).

3. Chan, C., Yin, H., Garforth, J., et al. Phenothiazine inhibitors of trypanothione reductase as potential antitrypanosomal and antileishmanial drugs. J. Med. Chem. 41(2), 148-156 (1998).

4. Ye, X., Linton, J.M., Schork, N.J., et al. A pharmacological network for lifespan extension in Caenorhabditis elegans. Aging Cell 13(2), 206-215 (2014).