BD-1063
Based on 3 publication(s) in Google Scholar
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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- No. CAS: 150208-28-9
- Fòrmula: C13H18Cl2N2
- Peso molecular:273.20
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) BD-1063
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Actividad biológica
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σ1R |
TRPC5 |
TRPM3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
>100 μM
Compound: BD, BD1063
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Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
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[PMID: 23415062] |
| MCF7 | EC50 |
70 μM
Compound: BD, BD1063
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Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay
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[PMID: 23415062] |
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 (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.
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Animal Model:CD-1 Mice with Inflammatory hyperalgesia (female, wild-type, 25-30 g, carrageenan-induced inflammatory hyperalgesia model)[3]
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Dosage:4 mg/kg; 8 mg/kg; 16 mg/kg
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Administration:s.c.; single dose
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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.
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Animal Model:Wistar (male, 300 g at study onset, alcohol dependence induced via intermittent 14-hour daily ethanol vapor exposure for 6 weeks)[4]
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Dosage:4.4 mg/kg; 7 mg/kg; 11 mg/kg
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Administration:s.c.; single dose (15 minutes before testing)
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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.
Chemical Information
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No. CAS 150208-28-9
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Peso molecular 273.20
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Fòrmula C13H18Cl2N2
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SMILES
ClC1=CC=C(C=C1Cl)CCN2CCN(C)CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Arch Toxicol
2024 Oct;98(10):3323-3336. PMID: 38896176 -
Neurobiol Dis
Sigma-1 receptor maintains ATAD3A as a monomer to inhibit mitochondrial fragmentation at the mitochondria-associated membrane in amyotrophic lateral sclerosis. [Abstract]2023 Apr:179:106031. PMID: 36736924 -
J Virol
SARS-CoV-2 NSP6 reduces autophagosome size and affects viral replication via sigma-1 receptor. [Abstract]2024 Nov 19;98(11):e0075424. PMID: 39445785
Pureza y Documentación
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BD-1063 Related Classifications
HY-18101 Related Classifications
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