BQ-788 钠盐

BQ-788 钠盐用途

BQ-788 sodium salt 是一种有效的，选择性的 ETB receptor 拮抗剂，能够抑制 ET-1 与人的 Girardi 心脏细胞结合，IC₅₀ 值为 1.2 nM；较弱地抑制人成神经细胞瘤 SK-N-MC 细胞中 ETA 受体，IC₅₀ 值为 1300 nM。

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BQ-788 钠盐名称

[ CAS 号 ]:
156161-89-6

[ 中文名 ]:
BQ-788 钠盐

[ 英文名 ]:
BQ-788 (sodium salt)

[英文别名 ]:

BQ 788
BQ-788 sodium salt
MFCD00797882
BQ-788 (sodium salt)

BQ-788 钠盐生物活性

[ 描述 ]:

BQ-788 sodium salt是一种有效,选择性的ETB 受体拮抗剂,在人类Girrardi心脏细胞中抑制ET-1与ETB受体结合的 IC50 为1.2 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 内皮素受体

研究领域 >> 心血管疾病

[ 靶点 ]

IC50: 1.2 nM (ETB)

[体外研究]

BQ-788有效且竞争性地抑制125I标记的ET-1与人Girrardi心脏细胞(hGH)中ETB受体的结合,IC50为1.2 nM,但仅很少抑制人神经母细胞瘤细胞系SK-中与ETA受体的结合。 N-MC细胞(IC50,1300nM)。 BQ-788显示高达10μM的激动活性并且竞争性地抑制由ETB选择性激动剂(pA2,8.4)诱导的血管收缩。 BQ-788还抑制ET-1的几种生物活性,如支气管收缩,细胞增殖和灌注ET-1的清除[1]。

[体内研究]

BQ-788(3mg/kg/h,iv)完全抑制药理学剂量的ET-1-或sarafotoxin6c(0.5nmol/kg,iv)诱导的ETB受体介导的抑制因子,但在清醒大鼠中没有升压反应。此外,BQ-788显着增加ET-1的血浆浓度,这被认为是体内潜在ETB受体阻断的指标。在Dahl盐敏感性高血压(DS)大鼠中,BQ-788(3mg/kg/h,iv)使血压增加约20mm Hg。据报道,BQ-788还可抑制ET-1诱导的支气管收缩,肿瘤生长和脂多糖诱导的器官衰竭[1]。 BQ 788(3 mg/kg)导致ET-1剂量反应曲线向左移动8倍,表明ETB扩张剂受体显着参与[2]。小鼠通过足底内用30nmol BQ-788治疗,减少机械痛觉过敏(47％和42％),热痛觉过敏(68％和76％),水肿(50％和30％);髓过氧化物酶活性(64％和32％),以及明显的疼痛行为。此外,使用clazosentan或BQ-788进行足底内治疗可减少脊髓(45％和41％)和外周(47％和47％)超氧阴离子的产生以及脊柱(47％和47％)和外周(33％和54％)脂质过氧化分别为[3]。

[参考文献]

[1]. Okada M, et al. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20(1):53-66.

[2]. Sargent CA, et al. Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S216-8.

[3]. Fattori V, et al. Differential regulation of oxidative stress and cytokine production by endothelin ETA and ETB receptors in superoxide anion-induced inflammation and pain in mice. J Drug Target. 2016 Oct 5:1-27

[相关活性小分子]

BQ-788 钠盐物理化学性质

[ 分子式 ]:
C₃₄H₅₀N₅NaO₇

[ 分子量 ]:
663.78000

[ 精确质量 ]:
663.36100

[ PSA ]:
161.90000

[ LogP ]:
4.59590

[ 储存条件 ]:
2-8℃

BQ-788 钠盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2923900090

BQ-788 钠盐海关

[ 海关编码 ]: 2923900090

[ 中文概述 ]:
2923900090 其他季铵盐及季铵碱。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:6.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2923900090 other quaternary ammonium salts and hydroxides。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%

BQ-788 钠盐文献

Endothelin-1 induces myofibrillar disarray and contractile vector variability in hypertrophic cardiomyopathy-induced pluripotent stem cell-derived cardiomyocytes.

J. Am. Heart Assoc. 3(6) , e001263, (2014)

Despite the accumulating genetic and molecular investigations into hypertrophic cardiomyopathy (HCM), it remains unclear how this condition develops and worsens pathologically and clinically in terms ...

Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy.

Am. J. Pathol. 184(11) , 3040-51, (2014)

Retinopathy of prematurity adversely affects premature infants because of oxygen-induced damage of the immature retinal vasculature, resulting in pathological neovascularization (NV). Our pilot studie...

Increased cerebrovascular sensitivity to endothelin-1 in a rat model of obstructive sleep apnea: a role for endothelin receptor B.

J. Cereb. Blood Flow Metab. 35(3) , 402-11, (2015)

Obstructive sleep apnea (OSA) is associated with cerebrovascular diseases. However, little is known regarding the effects of OSA on the cerebrovascular wall. We tested the hypothesis that OSA augments...

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