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Endomorphin 多肽
2025/2/11 16:50:21
内啡肽属于阿片类物质。该肽具有 4 位苯丙氨酸酰胺的修饰。1997 年,Zadina 等人发现了μ阿片受体(MOR)的内源性肽配体:内啡肽 1(Tyr1-Pro2-Trp3-Phe4-NH2,EM1)和内啡肽 2(Tyr1-Pro2-Phe3-Phe4-NH2,EM2)[1]。
内啡肽对 MOR 的亲和力最高,并且相对于所有已知的阿片类物质对δ和κ阿片受体系统具有极高的选择性[2][3]。
Endomorphin belongs to Opioid. The peptide has the modification: 4 Phe amide. The endogenous peptides ligands for μ opioid receptor (MOR), endomorphin 1 (Tyr1-Pro2-Trp3-Phe4-NH2, EM1) and endomorphin2 (Tyr1-Pro2-Phe3-Phe4-NH2, EM2) were discovered in 1997 by Zadina et al.[1].
EMs exhibit the highest affinity to the MOR and extraordinarily high selectivity relative to the δ and κ opioid receptor systems of all known opioid substances.[2][3]
单字母 H2N-YPWF-CONH2
多字母 H2N-Tyr-Pro-Trp-Phe-CONH2
氨基酸个数 4
分子式 C34H38N6O5
平均分子量(MW) 610.7
精确分子量(Exact Mass)(MW) 610.29
等电点(PI) -
pH=7.0时的净电荷数 1.97
GRAVY -0.15
亲水残基比例 -
消光系数 6990

溶解建议

参考文献:

1.Champion HC, Zadina JE, Kastin AJ, Hackler L, Ge LJ, Kadowitz PJ. Endomorphin 1 and 2, endogenous ligands for the mu-opioid receptor, decrease cardiac output, and total peripheral resistance in the rat. Peptides. 1997;18(9):1393-7.
2. Chu XP, Xu NS, Li P, Wang JQ. Endomorphin-1 and endomorphin-2, endogenous ligands for the mu-opioid receptor, inhibit electrical activity of rat rostral ventrolateral medulla neurons in vitro. Neuroscience. 1999;93(2):681-6.
3. Yu Y, Shao X, Wang CL, Liu HM, Cui Y, Fan YZ, Liu J, Wang R In vitro and in vivo characterization of opioid activities of endomorphins analogs with novel constrained C-terminus: evidence for the important role of proper spatial disposition of the third aromatic ring Peptides 2007 Apr;28(4):859-70

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