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GR 89696 fumarate

GR 89696 fumarate用途

GR 89696是一种高选择性κ2阿片受体激动剂,具有预防瘙痒的潜力[1]。

GR 89696 fumarate名称

[ CAS 号 ]:
126766-32-3

[ 英文名 ]:
GR 89696 fumarate

GR 89696 fumarate生物活性

[ 描述 ]:

GR 89696是一种高选择性κ2阿片受体激动剂,具有预防瘙痒的潜力[1]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

研究领域 >> 炎症/免疫

信号通路 >> 神经信号通路 >> 阿片受体

[体内研究]

GR 89696(肌肉注射,0.01-0.1μg/kg)可以以一种剂量依赖的方式减轻鞘内注射吗啡(0.03mg)诱导的抓挠反应而不影响吗啡镇痛作用[1]。 GR-896960(皮下注射,1 mg/kg)在大鼠永久性局灶性缺血模型中,使大脑动脉梗塞体积减少了 38%[2]。

[参考文献]

[1]. Mei-Chuan Ko, et al. Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates. J Pharmacol Exp Ther. 2009 Jan;328(1):193-200.

[2]. A Barber, et al. Effects of GR-89696 and the novel peripherally selective OP2 agonists, EMD-61569 and EMD-61747, against focal cerebral ischemia in the rat. Methods Find Exp Clin Pharmacol. 1999 Mar;21(2):105-13

GR 89696 fumarate物理化学性质

[ 沸点 ]:
559.2ºC at 760 mmHg

[ 分子式 ]:
C₂₃H₂₉Cl₂N₃O₇

[ 分子量 ]:
530.39800

[ 闪点 ]:
292ºC

[ 精确质量 ]:
529.13800

[ PSA ]:
127.69000

[ LogP ]:
2.43640

[ 蒸汽压 ]:
1.55E-12mmHg at 25°C

GR 89696 fumarate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

GR 89696 fumarate文献

[11C]GR103545: novel one-pot radiosynthesis with high specific activity.

Nucl. Med. Biol. 38(2) , 215-21, (2011)

GR103545 is a potent and selective kappa-opioid receptor agonist. Previous studies in non-human primates demonstrated favorable properties of [(11)C]GR103545 as a positron emission tomography tracer f...

GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys.

J. Pharmacol. Exp. Ther. 298(3) , 1049-59, (2001)

GR89,696 is a synthetic kappa-opioid receptor agonist, recently reported to have an agonist profile consistent with selectivity at the proposed "kappa(2)" subtype. The present studies evaluated the ef...

[(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers.

Nucl. Med. Biol. 29(1) , 47-53, (2002)

The R and S enantiomers of [(11)C]GR89696, [(11)C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate, were synthesized from their appropriate chiral precursors a...

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