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