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背景说明:Endomorphin 1,一种高度选择性的高亲和力μ-opioid受体激动剂 , 对kappa3结合位点具有高亲和力 ,Ki为 20 到 30 nM 之间。Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. In Vivo:Endomorphin 1 (i.c.v.) shows antinociceptive properties in mice, with an ED50 value of 6.16 nM. Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response. In Vitro:Endomorphin 1 inhibits Forskolin (HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells. Endomorphin 1 (1-10 μM) increases interleukin-8 secretion in Caco-2 cells. Endomorphin 1 (1 μM) inhibits excitatory transmission in adult rat substantia gelatinosa neurons. 参考文献:[1] Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.
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