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Men 10376

Men 10376用途

Men 10376 是一种有效的选择性的 tachykinin NK-2 受体拮抗剂,对大鼠小肠 NK-2 受体的 Ki 值为 4.4 μM。

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Men 10376名称

[ CAS 号 ]:
135306-85-3

[ 中文名 ]:
Men 10376

[ 英文名 ]:
(Tyr5,D-Trp6.8.9,Lys-NH2¹⁰)-Neurokinin A (4-10)

[英文别名 ]:

L-Asp-L-Tyr-D-Trp-L-Val-D-Trp-D-Trp-L-Lys-NH2
NK2 TACHYKININ RECEPT
M.W. 1081.24 C57H68N12O10
(TYR5,D-TRP6·8·9,LYS-NH210)-NEUROKININ A (4-10)
Men 10376

Men 10376生物活性

[ 描述 ]:

Men 10376 是一种有效的选择性的 tachykinin NK-2 受体拮抗剂,对大鼠小肠 NK-2 受体的 Ki 值为 4.4 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经激肽受体

信号通路 >> 神经信号通路 >> 神经激肽受体

多肽产品

研究领域 >> 其他

[ 靶点 ]

Ki: 4.4 μM (NK-2 receptor, rat small intestine)[1]

[体外研究]

男性10376是一种选择性速激肽NK-2受体,Ki为4.4μM,对NK-1和NK-3受体的选择性较低(Ki,>10μM)[1]。男性10376显示NK-1(豚鼠回肠)和NK-2受体(内皮剥夺的兔肺动脉)的pA2为5.66和8.08。男性10376对NK-3受体没有影响(Ki,>10μM)[2]。

[体内研究]

男性10376(1和3μmol/ kg)拮抗大鼠中NK-2受体激动剂产生的膀胱运动性增加[2]。

[参考文献]

[1]. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36.

[2]. Maggi CA, et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J Pharmacol Exp Ther. 1991 Jun;257(3):1172-8.

[相关活性小分子]

Men 10376物理化学性质

[ 密度 ]:
1.361 g/cm3

[ 沸点 ]:
1555.4ºC at 760 mmHg

[ 分子式 ]:
C₅₇H₆₈N₁₂O₁₀

[ 分子量 ]:
1081.22000

[ 闪点 ]:
894.5ºC

[ 精确质量 ]:
1080.52000

[ PSA ]:
374.63000

[ LogP ]:
6.53410

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0mmHg at 25°C

[ 折射率 ]:
1.672

[ 储存条件 ]:
-20°C

[ 水溶解性 ]:
Insuluble (2.3E-3 g/L) (25 ºC)

Men 10376MSDS

详细MSDS(安全技术说明书)

Men 10376安全信息

[ 危害码 (欧洲) ]:
N

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

[ WGK德国 ]:
3.0

Men 10376文献

Effects of substance P on identified neurons of the rat dorsal motor nucleus of the vagus.

Am. J. Physiol. Gastrointest. Liver Physiol. 281(1) , G164-72, (2001)

Previous evidence suggests that substance P (SP) activates subpopulations of neurons within the dorsal motor nucleus of the vagus (DMV). In this study we aimed at identifying these subpopulations in r...

Neurokinin receptors modulate the impact of uncontrollable stimulation on adaptive spinal plasticity.

Behav. Neurosci. 121(5) , 1082-94, (2007)

Previous research has demonstrated that spinally transected rats can acquire a prolonged flexion response to prevent the delivery of shock. However, rats that receive shock irrespective of leg positio...

Intrathecal administration of neurokinin 1 and neurokinin 2 receptor antagonists undermines the savings effect in spinal rats seen in an instrumental learning paradigm.

Behav. Neurosci. 121(1) , 186-99, (2007)

Research has demonstrated that the isolated spinal cord is capable of modifying its behavior in response to changes in environmental stimuli. Previous studies have shown that rats with complete thorac...

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