Benzquinamide hydrochloride  (Synonyms: P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride)

Benzquinamide (P2647; BZQ; Benzoquinamide) hydrochloride is an orally active binder of dopamine receptors and adrenergic receptors. Benzquinamide hydrochloride specifically targets dopamine D2, D3, D4 receptors and α-2A, α-2B, α-2C adrenergic receptors. Benzquinamide hydrochloride regulates blood pressure and heart rate, attenuates the pressor effect of adrenaline, and exhibits activities such as antiemesis, anxiolysis, and reduction of histamine-induced bronchoconstriction. Benzquinamide hydrochloride has good safety and does not deplete serotonin or norepinephrine in the brain. Benzquinamide hydrochloride can be used in studies related to nausea/vomiting, mental disorders, anxiety states, neurosis, and psychosis^[1][2].

Benzquinamide hydrochloride binds to human dopamine D₂, D₃, and D₄ receptors, with the highest affinity for the D₄ subtype (K_i=574 nM)^[1].
Benzquinamide hydrochloride (10 μM) binds to human α_2A, α_2B, and α_2C adrenergic receptors, with the highest affinity for the α_2C subtype (K_i=545 nM), and does not produce meaningful binding to histamine H1 receptors or muscarinic M1-M5 receptors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Benzquinamide (16.5 mg/kg; i.p.) hydrochloride specifically disrupts conditioned avoidance behavior in rats with an ED₅₀ of 16.5 mg/kg (i.p.), with 3.7-fold greater potency for disrupting avoidance than escape behavior^[2].
Benzquinamide (5-20 mg/kg; i.p.) hydrochloride inhibits isolation-induced fighting behavior in male mice starting at 5 mg/kg (i.p.) without causing muscle relaxation or impaired coordination^[2].
Benzquinamide (0.4-1.6 mg/kg; i.v.; 4.0-6.0 mg/kg; p.o.) hydrochloride blocks apomorphine-induced emesis in dogs with an intravenous ED₅₀ of approximately 0.9 mg/kg, and fully blocks emesis at 6.0 mg/kg (p.o.)^[2].
Benzquinamide (10-25 mg/kg; i.v.) hydrochloride does not deplete brain serotonin or norepinephrine concentrations in dogs at doses up to 25 mg/kg (i.v.)^[2].
Benzquinamide (10 mg/kg; i.v.) hydrochloride does not exhibit neuromuscular activity in Felis catus at 10 mg/kg (i.v.)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

440.96

C₂₂H₃₃ClN₂O₅

113-69-9

Solid

Off-white to light yellow

O=C(C1CN2CCC3=CC(OC)=C(OC)C=C3C2CC1OC(C)=O)N(CC)CC.[H]Cl

Room temperature in continental US; may vary elsewhere.

• [1]. Gregori-Puigjané E, et al. Identifying mechanism-of-action targets for drugs and probes. Proc Natl Acad Sci U S A. 2012;109(28):11178-11183.  [Content Brief]

  [2]. Scriabine A, et al. Benzquinamide: a new antianxiety drug[J]. JAMA, 1963, 184(4): 276-279.