Adenosine A1 receptor activator T62

Adenosine A1 receptor activator T62用途

Adenosine A1 receptor activator T62 是腺苷 A1 受体 (adenosine A1 receptor) 的变构增强剂。Adenosine A1 receptor activator T62 在急性疼痛的动物模型中产生抗伤害感受,并在炎性和神经损伤性疼痛的模型中降低超敏反应。

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Adenosine A1 receptor activator T62名称

[ CAS 号 ]:
40312-34-3

[ 中文名 ]:
T62

[ 英文名 ]:
T62

[英文别名 ]:

UNII-9Q765ZIF8L
T62

Adenosine A1 receptor activator T62生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

[ 靶点 ]

Adenosine A1 receptor[1]

[体内研究]

腺苷A1受体激活剂T62(0.3-3μg；鞘内给药；雄性SpragueDawley大鼠)治疗产生剂量依赖性抗过敏作用,对行走或活动水平无影响[1]。动物模型：雄性SpragueDawley大鼠(250g)足爪切开术后[1]剂量：0.3μg,0.5μg,1μg,3μg给药：鞘内给药结果：产生剂量依赖性抗过敏作用,对行走和活动水平无影响。ED40(95%可信区间)为0.77(0.63-0.91)μg。

[参考文献]

[1]. Obata H, et al. Spinal adenosine receptor activation reduces hypersensitivity after surgery by a different mechanism than after nerve injury. Anesthesiology. 2004 May;100(5):1258-62.

[2]. Li X, et al. Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism. J Pharmacol Exp Ther. 2003 Jun;305(3):950-5.

[3]. Soudijn W, et al. Allosteric modulation of G protein-coupled receptors: perspectives and recent developments. Drug Discov Today. 2004 Sep 1;9(17):752-8.

Adenosine A1 receptor activator T62物理化学性质

[ 密度 ]:
1.337g/cm3

[ 沸点 ]:
527ºC at 760 mmHg

[ 分子式 ]:
C₁₅H₁₄ClNOS

[ 分子量 ]:
291.79600

[ 闪点 ]:
272.5ºC

[ 精确质量 ]:
291.04800

[ PSA ]:
71.33000

[ LogP ]:
4.67470

[ 折射率 ]:
1.658

[ 储存条件 ]:
2-8°C，密封，干燥

Adenosine A1 receptor activator T62MSDS

详细MSDS(安全技术说明书)

Adenosine A1 receptor activator T62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

[ WGK德国 ]:
3

[ 海关编码 ]:
2934999090

Adenosine A1 receptor activator T62合成路线

详细合成路线

Adenosine A1 receptor activator T62上下游产品

Adenosine A1 receptor activator T62上游产品

Adenosine A1 receptor activator T62下游产品

Adenosine A1 receptor activator T62海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Adenosine A1 receptor activator T62文献

Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism.

J. Pharmacol. Exp. Ther. 305 , 950-955, (2003)

Activation of adenosine A1 receptors by endogenous adenosine or synthetic agonists produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory a...

Repeated dosing with oral allosteric modulator of adenosine A1 receptor produces tolerance in rats with neuropathic pain.

Anesthesiology 100(4) , 956-61, (2004)

The positive allosteric adenosine receptor modulator, T62 (2-amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophene), has been shown to reduce mechanical allodynia in a rat model of neuropathic pa...

Allosteric modulation of G protein-coupled receptors: perspectives and recent developments.

Drug Discov. Today 9 , 752-758, (2004)

Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach to gain selectivity in drug action. In this overview, allosteric modulators that enhance or...

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