Benzquinamide (hydrochloride)

Benzquinamide is an antiemetic and antagonist of dopamine D2-, D4-, and D3 receptors (Kis = 4,369, 574, and 3,592 nM, respectively). It is also an antagonist of alpha2-adrenergic receptors (alpha2-ARs, Kis = 1,365, 691, and 545 nM for alpha2A-, alpha2B-, and alpha2C-AR, respectively). Benzquinamide has been mistakenly identified as an antagonist of histamine H1 receptors and M1-5 muscarinic acetylcholine receptors (mAChRs). It inhibits conditioned avoidance in the shuttle box test in dogs (ED50 = 2.77 mg/kg). Benzquinamide inhibits apomorphine-induced emesis in dogs (ED50 = 0.69 mg/kg). It induces tachycardia, increases blood levels of norepinephrine, and temporarily decreases systolic and diastolic blood pressure, which revert to baseline within one minute, in normotensive dogs when administered at doses ranging from 0.5 to 5 mg/kg. Formulations containing benzquinamide have previously been used as antiemetics following surgery or anesthesia.Formal Name: 2-(acetyloxy)-N,N-diethyl-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-2H-Benzo[a]quinolizine-3-carboxamide, monohydrochloride. CAS Number: 113-69-9. Molecular Formula: C22H32N2O5 . HCl. Formula Weight: 441.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-10 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: CCN(C(C1C(OC(C)=O)CC2N(CCC3=CC(OC)=C(C=C32)OC)C1)=O)CC.Cl. InChi Code: InChI=1S/C22H32N2O5.ClH/c1-6-23(7-2)22(26)17-13-24-9-8-15-10-20(27-4)21(28-5)11-16(15)18(24)12-19(17)29-14(3)25,/h10-11,17-19H,6-9,12-13H2,1-5H3,1H. InChi Key: KZLNXGBVFTWMPS-UHFFFAOYSA-N.