D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2(DISULFIDE BRIDGE:CYS2-PEN7)

用途

CTAP 是一种强效、高选择性的脑渗透类阿片受体 (μ opioid receptor)拮抗剂 (IC50=3.5 nM),对 δ opioid受体 (IC50=4500 nM) 和生长抑素受体具有超过 1200 倍的选择性。CTAP 可用于 L -多巴胺 (HY-N0304) 诱导的运动障碍 (LID) 的研究。

名称

[ CAS 号 ]:
103429-32-9

[ 中文名 ]:
D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2(DISULFIDE BRIDGE:CYS2-PEN7)

[ 英文名 ]:
H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (Disulfide bond between Cys2 and Pen7)

[英文别名 ]:

CYS2,TYR3,ARG5,PEN7-AMIDE
M.W. 1104.30 C51H69N13O11S2
cyclic D-Pen-Cys-Tyr-D-Trp-Arg-ThrPen-Thr-NH2
H-D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 3.5 nM (μ opioid receptor) IC50: 4500 nM (δ opioid receptor)[1]

[参考文献]

[1]. Mitchell J Bartlett, et al. Highly-selective µ-opioid Receptor Antagonism Does Not Block L-DOPA-induced Dyskinesia in a Rodent Model.BMC Res Notes

物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 分子式 ]:
C₅₁H₆₉N₁₃O₁₁S₂

[ 分子量 ]:
1104.304

[ 精确质量 ]:
1103.468140

[ PSA ]:
461.79000

[ LogP ]:
0.44

[ 外观性状 ]:
白色固体/粉末

[ 折射率 ]:
1.699

[ 储存条件 ]:
-20°C

MSDS

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

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

[ WGK德国 ]:
3.0

合成路线

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文献

Buprenorphine decreases the CCL2-mediated chemotactic response of monocytes.

J. Immunol. 194(7) , 3246-58, (2015)

Despite successful combined antiretroviral therapy, ∼ 60% of HIV-infected people exhibit HIV-associated neurocognitive disorders (HAND). CCL2 is elevated in the CNS of infected people with HAND and me...

Effect of μ-opioid agonist DAMGO on surface CXCR4 and HIV-1 replication in TF-1 human bone marrow progenitor cells.

BMC Res. Notes 7 , 752, (2014)

Approximately one-third of the AIDS cases in the United States have been attributed to the use of injected drugs, frequently involving the abuse of opioids. Consequently, it is critical to address whe...

Dopamine/Tyrosine Hydroxylase Neurons of the Hypothalamic Arcuate Nucleus Release GABA, Communicate with Dopaminergic and Other Arcuate Neurons, and Respond to Dynorphin, Met-Enkephalin, and Oxytocin.

J. Neurosci. 35 , 14966-82, (2015)

We employ transgenic mice with selective expression of tdTomato or cre recombinase together with optogenetics to investigate whether hypothalamic arcuate (ARC) dopamine/tyrosine hydroxylase (TH) neuro...

更多文献

D-PHE-CYS-TYR-D-TRP-ARG-THR-PEN-THR-NH2(DISULFIDE BRIDGE:CYS2-PEN7)

用途

名称

生物活性

物理化学性质

MSDS

详细MSDS(安全技术说明书)

安全信息

合成路线

详细合成路线

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文献

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