Benzquinamide (hydrochloride)

Benzquinamide is an antiemetic and antagonist of dopamine D₂-, D₄-, and D₃ receptors (K_is = 4,369, 574, and 3,592 nM, respectively).¹ It is also an antagonist of α₂-adrenergic receptors (α₂-ARs; K_is = 1,365, 691, and 545 nM for α_2A-, α_2B-, and α_2C-AR, respectively). Benzquinamide has been mistakenly identified as an antagonist of histamine H₁ receptors and M_1-5 muscarinic acetylcholine receptors (mAChRs). It inhibits conditioned avoidance in the shuttle box test in dogs (ED₅₀ = 2.77 mg/kg).² 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.³ Formulations containing benzquinamide have previously been used as antiemetics following surgery or anesthesia.

WARNING This product is not for human or veterinary use.

1. Gregori-Puigjané, E., Setola, V., Hert, J., et al. Identifying mechanism-of-action targets for drugs and probes. Proc. Natl. Acad. Sci. USA 109(28), 11178-11183 (2012).

2. Niemegeers, C.J.E. Antiemetic specificity of dopamine antagonists. Psychopharmacology (Berl.) 78(3), 210-213 (1982).

3. Smith, D.J., Rushin, J.M., Urquilla, P.R., et al. Cardiovascular effects of benzquinamide. Anesth. Analg. 58(3), 189-194 (1979).