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 ?M.^4,3 Propionylpromazine inhibits recombinant T. cruzi trypanothione reductase (IC₅₀ = 357 ?M) and is active against T. brucei trypomastigotes (ED50 = 10.1 ?M) but not L. donovani amastigotes or T. cruzi trypomastigotes (ED₅₀s = >30 ?M) 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.

1.Fielding, S., and Lal, H.Biochemical actions of neuroleptic drugs: focus on the dopamine receptorHandbook of psychopharmacology37-55(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 analysesInsect Biochem. Molec.42(11)846-853(2012) 3.Meyer, J.M., Ejendal, K.F.K., Avramova, L.V., et al.A "genome-to-lead" approach for insecticide discovery: pharmacological characterization and screening of Aedes aegypti D(1)-like dopamine receptorsPlos Negl. Trop. D.6(1)e1478(2012) 4.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 analysesInsect Biochem. Molec.42(11)846-853(2012) 5.Chan, C., Yin, H., Garforth, J., et al.Phenothiazine inhibitors of trypanothione reductase as potential antitrypanosomal and antileishmanial drugsJ. Med. Chem.41(2)148-156(1998) 6.Ye, X., Linton, J.M., Schork, N.J., et al.A pharmacological network for lifespan extension in Caenorhabditis elegansAging Cell13(2)206-215(2014)