Promethazine (hydrochloride)

Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors^[1][2].
In Vitro:Promethazine hydrochloride (1.25-10 μM, 3 days) inhibits adipocyte formation in a dose-dependent manner^[1].
Promethazine hydrochloride (10 μM, 0-12 days) decreases the expression of peroxisome proliferator activated receptor γ (PPARG) and reduces the phosphorylation level of CREB in PDGFRα⁺ cells^[1].
Promethazine hydrochloride (10-1000 μM, 1-24 h) has cytotoxic at concentrations greater than 100 μM in L929 lung fibroblast cells^[3].
In Vivo:Promethazine hydrochloride (0.05-0.1 mg/mL, p.o., 4 weeks) possesses inhibitory effect on ectopic fat cell formation in skeletal muscle in a mouse achilles tendon rupture model^[1].
Promethazine hydrochloride (2.4-9.6 mg/kg, p.o.) has no effect on the development of femoral osteoporosis and retarded normal femoral expansion in the adult castrate male rats^[4].