2. Neuronal Signaling Membrane Transporter/Ion Channel
  3. Sigma Receptor TRP Channel
  4. BD-1063

BD-1063 是一种选择性 σ-1 受体拮抗剂，并对 TRPC5 和 TRPM3 具有抑制活性。BD-1063 通过抑制 TRPC5 和 TRPM3 介导的持续性钙内流，发挥抗痛觉过敏和抗异常性疼痛的作用，并能逆转 Carrageenan (HY-125474) 的作用。BD-1063 还能显著减少过度的乙醇自我给药行为。BD-1063 被广泛应用于神经性疼痛、炎性痛觉过敏以及酒精滥用与依赖的相关机制研究。

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BD-1063

BD-1063 Chemical Structure

CAS No. : 150208-28-9

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BD-1063 的其他形式现货产品:

Other Forms of BD-1063:

BD-1063 相关抗体

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

BD-1063 (10-100 μM; 30 min) 可抑制组胺、VEGF 或 H2O2 在人大隐静脉内皮细胞中诱发的持续性钙内流，其作用独立于 Sigma-1 受体，有效浓度分别为 10、50 和 100 μM[2]。
BD-1063 (100 μM; 30 min 或 1 h) 可抑制 HEK 293 细胞中过表达的 TRPC5 或 TRPM3 通道介导的钙内流[2]。

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

BD-1063 相关抗体:
体内研究
(In Vivo)

BD-1063 (5.6-56.2 mg/kg；皮下注射) 在大鼠 CCI 神经病理性疼痛模型中产生剂量依赖性的抗痛觉过敏和抗异常性疼痛作用，其抗痛觉过敏的 ED50 值为 28.8 mg/kg，抗异常性疼痛的 ED50 值为 18.2 mg/kg；并与 Quercetin hydrate (HY-18085A) 具有协同作用[1]。
BD-1063 (4-16 mg/kg；皮下注射) 可通过 σ1 受体介导的机制完全逆转 Carrageenan (HY-125474) 诱导的野生型 CD-1 小鼠炎症性机械痛觉过敏和热痛觉过敏，其 ED50 值分别为 4 mg/kg 和 6 mg/kg，且不会影响未发炎小鼠的伤害性疼痛[3]。
BD-1063 (25-75 μg/paw；足底注射) 可通过 σ1 受体介导的机制完全逆转野生型 CD-1 小鼠中 Carrageenan (HY-125474) 诱导的机械性痛觉和热痛觉过敏，且无全身效应[3]。
BD-1063 (4.4-11 mg/kg；皮下注射) 可呈剂量依赖性地减少急性戒断期乙醇依赖雄性 Wistar 大鼠的乙醇自我给药行为，其中 11 mg/kg 剂量可对所有受试对象产生显著的抑制作用[4]。
BD-1063 (3-11 mg/kg；皮下注射) 可剂量依赖性地降低经基因筛选的雄性撒丁岛嗜酒大鼠的乙醇自主摄取量，在 4.4 mg/kg 及更高剂量下可观察到显著的抑制作用[4]。

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.
分子量

273.20

Formula

C13H18Cl2N2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BD-1063 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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