2. Neuronal Signaling Membrane Transporter/Ion Channel
  3. Sigma Receptor TRP Channel
  4. 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.

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BD-1063

BD-1063 Chemical Structure

CAS No. : 150208-28-9

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TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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Description

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].

IC50 & Target[2]

σ1R

 

TRPC5

 

TRPM3

 

In Vitro

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 Related Antibodies
In Vivo

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.

Animal Model: CD-1 Mice with Inflammatory hyperalgesia (female, wild-type, 25-30 g, carrageenan-induced inflammatory hyperalgesia model)[3]
Dosage: 4 mg/kg; 8 mg/kg; 16 mg/kg
Administration: s.c.; single dose
Result: Dose-dependently reversed inflammatory mechanical and thermal hyperalgesia, increasing response latencies to levels close to noninflamed control mice.
Achieved an ED50 of 4 mg/kg for reversing mechanical hyperalgesia.
Achieved an ED50 of 6 mg/kg for reversing thermal hyperalgesia.
Reached a maximum antihyperalgesic effect (Emax) not significantly different from 100% recovery for both sensory modalities.
Did not alter response latencies in noninflamed mice at doses that fully reversed hyperalgesia (8 mg/kg for mechanical, 16 mg/kg for thermal).
Had antihyperalgesic effects completely abolished by subcutaneous administration of the σ1 agonist PRE-084 in a dose-dependent manner.
Animal Model: Wistar (male, 300 g at study onset, alcohol dependence induced via intermittent 14-hour daily ethanol vapor exposure for 6 weeks)[4]
Dosage: 4.4 mg/kg; 7 mg/kg; 11 mg/kg
Administration: s.c.; single dose (15 minutes before testing)
Result: Reduced ethanol self-administration in a dose-dependent manner.
Significantly reduced ethanol intake and lever press responses relative to vehicle at 7 mg/kg and 11 mg/kg doses.
Reduced ethanol self-administration by 49% in low-responding dependent rats and 34% in high-responding dependent rats.
Did not alter concurrent water self-administration.
Molecular Weight

273.20

Formula

C13H18Cl2N2
CAS No.
SMILES

ClC1=CC=C(C=C1Cl)CCN2CCN(C)CC2
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BD-1063150208-28-9BD1063BD 1063Sigma ReceptorTRP ChannelTransient receptor potential channelshuman saphenous vein endothelial cellswild-type CD-1 micesigma-1 receptorσ 1 -KO CD-1 micemale Wistar ratsmale Sardinian alcohol-preferring ratsTRPC5TRPM3HEK 293 cellsrat CCI neuropathic pain model
Inhibitorinhibitorinhibit

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