Droperidol

Droperidol is a dopamine D2 and D4 receptor antagonist (Kis = 0.25 and 0.84 nM for human D2 and D4 receptors, respectively). It also inhibits the voltage-gated potassium channel hERG, also known as Kv11.1 (IC50 = 32 nM), and binds to the serotonin (5-HT) receptor subtype 5-HT2 (Ki = 1.1 nM). Droperidol (1, 5, and 10 µM) decreases action potential duration in isolated canine Purkinje fibers. It prevents apomorphine-induced vomiting in dogs (ED50 = 0.0012 mg/kg) and induces catalepsy in rats (ED50 = 0.13 mg/kg). Formulations containing droperidol have been used in the treatment of surgery-associated nausea and vomiting.Formal Name: 1-[1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl]-1,3-dihydro-2H-benzimidazol-2-one. CAS Number: 548-73-2. Synonyms: DHBP, NSC 169874. Molecular Formula: C22H22FN3O2. Formula Weight: 379.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 233, 282 nm. SMILES: FC1=CC=C(C(CCCN2CC=C(N3C(NC4=C3C=CC=C4)=O)CC2)=O)C=C1. InChi Code: InChI=1S/C22H22FN3O2/c23-17-9-7-16(8-10-17)21(27)6-3-13-25-14-11-18(12-15-25)26-20-5-2-1-4-19(20)24-22(26)28/h1-2,4-5,7-11H,3,6,12-15H2,(H,24,28). InChi Key: RMEDXOLNCUSCGS-UHFFFAOYSA-N.