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编 号:F161235
分子式:C96H140N20O25S
分子量:2006.32
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生物活性:
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.

体内研究:
BQ-3020 (3 mg/kg 皮下注射, 单次给药) 可使癌痛小鼠模型在注射后 3 小时内的癌痛减轻约 50%。Animal Model:Cancer pain mouse model
Dosage:3 mg/kg
Administration:Injected subcutaneously at the site of the greatest tumor development
Result:Attenuated cancer pain by approximately 50% up to 3 h post-injection compared to PBS-vehicle and contralateral injection

体外研究:
BQ-3020(0.01–300 nM,7分钟)对 PhE 预收缩的尿路上皮剥离组织产生浓度依赖性松弛。BQ-3020 (0.01–200 nM,20 min) 通过抑制 ETB 受体引起兔肺动脉剂量依赖性血管收缩,其 EC50 值为 0.57 nM。
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