1,6-双(环己基脒基羰基氨基)己烷

1,6-双(环己基脒基羰基氨基)己烷用途

RHC 80267 (U-57908) 是一种有效的选择性二酰基甘油脂酶 (DAGL) 抑制剂 (对犬血小板的 IC50 为 4 μM)。RHC 80267 抑制胆碱酯酶活性,IC50 为 4 μM,从而增强了乙酰胆碱引起的松弛。RHC 80267 还抑制 COX 活性和磷脂酰胆碱的水解。

1,6-双(环己基脒基羰基氨基)己烷名称

[ CAS 号 ]:
83654-05-1

[ 中文名 ]:
1,6-双(环己基脒基羰基氨基)己烷

[ 英文名 ]:
RHC-80267

[英文别名 ]:

1,6-Bis-cyclohexylidenaminooxycarbonylamino-hexan
1,6-bis-cyclohexylidenaminooxycarbonylamino-hexane

1,6-双(环己基脒基羰基氨基)己烷生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

信号通路 >> 免疫及炎症 >> COX

研究领域 >> 代谢疾病

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 4 μM (Canine diacylglycerol lipase), 4 μM (Cholinesterase); COX; Phosphatidylcholine[1][3][4]

[体外研究]

RHC 80267对乙酰胆碱的舒张作用增强可能是由于胆碱酯酶的抑制作用：(1)rhc80267对乙酰胆碱的氨甲酰衍生物卡巴胆碱的反应没有影响,卡巴胆碱与乙酰胆碱的区别在于它对胆碱酯酶水解的抵抗力,并且(2)模拟了rhc80267的作用通过胆碱酯酶新斯的明抑制剂,RHC 80267在新斯的明的最大有效浓度存在下不显示额外的效果。测定RHC 80267对脑匀浆胆碱酯酶活性的影响,证实rhc80267在相同浓度范围内抑制这种酶,增加对乙酰胆碱的松弛,即在1-10μM时[2]。

[体内研究]

RHC 80267(40μM)以内皮依赖的方式增强U46619(血栓素A2类似物)和血管紧张素II(ANG II)在人和大鼠肺动脉(分别为hPAs和rPAs)中诱导的收缩[3]。

[参考文献]

[1]. Sutherland CA, et al. Relative activities of rat and dog platelet phospholipase A2 and diglyceride lipase. Selective inhibition of diglyceride lipase by RHC 80267. J Biol Chem. 1982 Dec 10;257(23):14006-10.

[2]. Ghisdal P, et al. The diacylglycerol lipase inhibitor RHC-80267 potentiates the relaxation to acetylcholine in rat mesenteric artery by anti-cholinesterase action. Eur J Pharmacol. 2005 Jul 4;517(1-2):97-102.

[3]. Karpińska O, et al. Activation of CB1 receptors by 2-arachidonoylglycerol attenuates vasoconstriction induced by U46619 and angiotensin II in human and rat pulmonary arteries. Am J Physiol Regul Integr Comp Physiol. 2017 Jun 1;312(6):R883-R893.

[4]. Oglesby TD, et al. The inhibition of arachidonic acid metabolism in human platelets by RHC 80267, a diacylglycerol lipase inhibitor. Biochim Biophys Acta. 1984 Apr 18;793(2):269-77.

1,6-双(环己基脒基羰基氨基)己烷物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 分子式 ]:
C₂₀H₃₄N₄O₄

[ 分子量 ]:
394.508

[ 精确质量 ]:
394.257996

[ PSA ]:
101.38000

[ LogP ]:
3.12

[ 外观性状 ]:
白色固体

[ 折射率 ]:
1.571

[ 储存条件 ]:
2-8°C，避光，干燥，密封

1,6-双(环己基脒基羰基氨基)己烷MSDS

详细MSDS(安全技术说明书)

1,6-双(环己基脒基羰基氨基)己烷安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
22-24/25

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

1,6-双(环己基脒基羰基氨基)己烷合成路线

详细合成路线

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1,6-双(环己基脒基羰基氨基)己烷文献

Capsazepine, a vanilloid antagonist, abolishes tonic responses induced by 20-HETE on guinea pig airway smooth muscle.

Am. J. Physiol. Lung Cell. Mol. Physiol. 288(3) , L460-70, (2005)

The aim of this study was to delineate the mode of action of 20-hydroxy-eicosatetraenoic acid (20-HETE) in airway smooth muscle (ASM) cells. ASM metabolizes arachidonic acid by various enzymatic pathw...

L- and N-current but not M-current inhibition by M1 muscarinic receptors requires DAG lipase activity.

J. Cell Physiol. 216(1) , 91-100, (2008)

Stimulation of postsynaptic M(1) muscarinic receptors (M(1)Rs) increases firing rates of both sympathetic and central neurons that underlie increases in vasomotor tone, heart rate, and cognitive memor...

Brain phospholipase C-diacylglycerol lipase pathway is involved in vasopressin-induced release of noradrenaline and adrenaline from adrenal medulla in rats.

Eur. J. Pharmacol. 499(1-2) , 99-105, (2004)

Recently, we reported that intracerebroventricularly (i.c.v.) administered arginine-vasopressin evokes the release of noradrenaline and adrenaline from adrenal medulla by brain thromboxane A2-mediated...

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