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60117-24-0

中文名称 TYR-GLY-GLY-PHE-LEU-NH2
CAS 60117-24-0
分子式 C28H38N6O6
分子量 554.64
MOL 文件 60117-24-0.mol
更新日期 2024/06/02 19:54:12
60117-24-0 结构式 60117-24-0 结构式

基本信息

中文别名
2-[[2-[[2-[[2-[[2-AMINO-3-(4-HYDROXYPHENYL)PROPANOYL]AMINO]ACETYL]AMINO]ACETYL]AMINO]-3-PHENYLPROPANOYL]AMINO]-4-METHYLPENTANAMIDE
英文别名
YGGFL-NH2
NSC 351912
LEU-ENKEPHALIN NH2
enkephalinamide-leu
LEU-ENKEPHALIN AMIDE
[LEU5]-ENKEPHALIN AMIDE
DYNORPHIN A (1-5) AMIDE
TYR-GLY-GLY-PHE-LEU-NH2
leucine enkephalinamide
H-TYR-GLY-GLY-PHE-LEU-NH2

物理化学性质

熔点123-126 °C
沸点1012.8±65.0 °C(Predicted)
密度1.254±0.06 g/cm3(Predicted)
储存条件−20°C
酸度系数(pKa)9.97±0.15(Predicted)

安全数据

WGK Germany3

常见问题列表

生物活性
[Leu5]-Enkephalin, amide 是一种 δ 阿片受体 (opioid receptor) 激动剂。
靶点

δ opioid receptor

体外研究

[Leu5]-Enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC 50 value of 2.1 nM.

体内研究

Levels of [Leu5]-Enkephalin are significantly increased in the nucleus raphe magnus (NRM) of rats 2 weeks after the injection of complete Freund's adjuvant (CFA) (1.02±0.2 pmol/mg protein) as compared with saline-treated rats (0.49±0.04 pmol/mg protein; p<0.01). Tissue levels of [Leu5]-Enkephalin are uniformly increased in the caudal ventrolateral periaqueductal gray (PAG) 4 hr (1.15±0.25 pmol/mg protein), 4 d (1.16±0.18 pmol/mg protein), and 2 weeks (1.18±0.17 pmol/mg protein) after the injection of CFA as compared with saline-treated rats (0.55±0.03 pmol/mg protein; p<0.05, all times). A smaller increase in the levels of [Leu5]-Enkephalin occurred in the rostral aspect of the ventrolateral PAG at all time points. Finally, levels of [Leu5]-Enkephalin are also increased in the contralateral microcellular tegmental nucleus 4 d after the injection of CFA (0.53±0.04 pmol/mg protein) compared with levels in saline-treated rats (0.38±0.02 pmol/mg protein; p<0.05).

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