BD-1063 

BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence^[1][2][3][4].

BD-1063 (10-100 μM; 30 min) inhibits sustained calcium entry evoked by histamine, VEGF, or H₂O₂ in human saphenous vein endothelial cells, acting independently of the Sigma-1 receptor, with effective concentrations of 10, 50, and 100 μM^[2].
BD-1063 (100 μM; 30 min) inhibits calcium influx through TRPC5 channels overexpressed in HEK 293 cells^[2].

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

BD-1063 (5.6-56.2 mg/kg; subcutaneous administration) produces dose-dependent anti-allodynic and anti-hyperalgesic effects in a rat CCI neuropathic pain model, with an ED₅₀ value of 28.8 mg/kg for anti-hyperalgesia and 18.2 mg/kg for anti-allodynia; it also exerts a synergistic effect with Quercetin hydrate (HY-18085A)^[1].
BD-1063 (4-16 mg/kg; subcutaneous injection) completely reverses carrageenan (HY-125474)-induced inflammatory mechanical hyperalgesia and thermal hyperalgesia in wild-type CD-1 mice via a σ₁ receptor-mediated mechanism, with ED₅₀ values of 4 mg/kg and 6 mg/kg, respectively, and does not affect nociceptive pain in non-inflamed mice^[3].
BD-1063 (25-75 μg/paw; intraplantar injection) fully reverses carrageenan (HY-125474)-induced mechanical hyperalgesia and thermal hyperalgesia in wild-type CD-1 mice via a σ₁ receptor-mediated mechanism, without producing systemic effects^[3].
BD-1063 (4.4-11 mg/kg; subcutaneous injection) reduces ethanol self-administration behavior in male Wistar rats with ethanol dependence during acute withdrawal in a dose-dependent manner, and the 11 mg/kg dose produces significant inhibitory effects in all test subjects^[4].
BD-1063 (3-11 mg/kg; subcutaneous injection) reduces ethanol self-administration in genetically selected male Sardinian alcohol-preferring rats in a dose-dependent manner, with significant inhibitory effects observed at doses of 4.4 mg/kg and higher^[4].

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

273.20

C₁₃H₁₈Cl₂N₂

150208-28-9

ClC1=CC=C(C=C1Cl)CCN2CCN(C)CC2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Espinosa-Juárez JV, et al. Sigma-1 receptor antagonist (BD-1063) potentiates the antinociceptive effect of quercetin in neuropathic pain induced by chronic constriction injury. Drug Dev Res. 2021;82(2):267-277.

  [2]. Amer MS, et al. Inhibition of endothelial cell Ca²⁺ entry and transient receptor potential channels by Sigma-1 receptor ligands. Br J Pharmacol. 2013;168(6):1445-1455.  [Content Brief]

  [3]. Tejada MA, et al. Sigma-1 receptor inhibition reverses acute inflammatory hyperalgesia in mice: role of peripheral sigma-1 receptors. Psychopharmacology (Berl). 2014;231(19):3855-3869.

  [4]. Sabino V, et al. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology. 2009;34(6):1482-1493.  [Content Brief]