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ACETYL-(ALA11·15)-ENDOTHELIN-1 (6-21)

用途

BQ-3020是一种选择性内皮素受体(ETB受体)激动剂,可取代与ETB受体结合的[125I]ET-1,IC50值为0.2 nM。BQ-3020引起兔肺动脉血管收缩。BQ-3020使猪膀胱颈松弛,可用于心血管疾病研究12。

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名称

[ CAS 号 ]:
143113-45-5

[ 中文名 ]:
ACETYL-(ALA11·15)-ENDOTHELIN-1 (6-21)

[ 英文名 ]:
Acetyl-(Ala11.15)-Endothelin-1 (6-21) ammonium salt

[英文别名 ]:

N-Acetyl-[Ala11,15]-Endothelin 1 fragment 6-21
MFCD00214633
Acetyl-(Ala 11,15)-ET 1 (6-21)

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 内皮素受体

[ 靶点 ]

ETB:0.2 nM (IC50)

[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[1] BQ-3020(0.01–200 nM,20分钟)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 0.57nM[2]

[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%[3]动物模型：癌症疼痛小鼠模型[3]剂量：3 mg/kg给药：在肿瘤发展最严重的部位皮下注射结果：与PBS-载体和对侧注射相比,注射后3小时癌症疼痛减轻约50%

[参考文献]

[1]. Arteaga JL,et.al. Endothelin ET(B) receptors are involved in the relaxation to the pig urinary bladder neck. Neurourol Urodyn. 2012 Jun;31(5):688-94.

[2]. Ihara M, et.al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 1992;51(6):PL47-52.

[3]. Quang PN, et.al. Peripheral endothelin B receptor agonist-induced antinociception involves endogenous opioids in mice. Pain. 2010 May;149(2):254-262.

物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
2125.8±65.0 °C at 760 mmHg

[ 分子式 ]:
C₉₆H₁₄₀N₂₀O₂₅S

[ 分子量 ]:
2006.32

[ 闪点 ]:
1239.5±34.3 °C

[ 精确质量 ]:
2005.001953

[ PSA ]:
730.82000

[ LogP ]:
6.02

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.582

安全信息

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

文献

Endothelin-1 stimulates aldosterone synthesis in Conn's adenomas via both A and B receptors coupled with the protein kinase C- and cyclooxygenase-dependent signaling pathways.

J. Investig. Med. 48(5) , 343-50, (2000)

The mechanisms and factors leading to enhanced aldosterone secretion and ultimately to neoplastic transformation of the adrenal cortex are poorly defined. Angiotensin-II (Ang-II) and endothelin-1 (ET-...

Marked reduction of mortality in salt-loaded Dahl salt-sensitive rats by the new, selective endothelin ETA receptor antagonist, J-105859.

J. Hypertens. 18(12) , 1815-23, (2000)

To examine the chronic effects of a newly synthesized, potent and selective endothelin (ET) ETA receptor antagonist, J-1 05859, on mortality in salt-loaded Dahl salt-sensitive (DS) rats and to confirm...

Mechanisms involved in the effects of endothelin-1 in pig prostatic small arteries.

Eur. J. Pharmacol. 640(1-3) , 190-6, (2010)

Since endothelin-1 (ET-1) is involved in prostatic disorders, the current study investigated the mechanisms underlying the ET-1-induced effects in pig prostatic small arteries. The experiments were pe...

更多文献

ACETYL-(ALA11·15)-ENDOTHELIN-1 (6-21)

用途

名称

生物活性

物理化学性质

安全信息

文献

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