EndoMor-phin 2，一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。EndoMor-phin 2, 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 Vitro
EndoMor-phin 2 is an endogenous opioid peptide and one of the two EndoMor-phins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with EndoMor-phin 1 (EM-2). The two EndoMor-phins display reasonable affinities for kappa3 binding sites, with Ki values between 20 and 30 nM. EndoMor-phin 1 and EndoMor-phin 2 compete both μ1 and μ2 receptor sites quite potently. EndoMor-phins have little appreciable affinity for either delta or kappa1 binding sites, with Ki values greater than 500 nM.
In Vivo
Both EndoMor-phin 1 and EndoMor-phin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. EndoMor-phin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than EndoMor-phin 2. The response of both agents are readily reversed by nalo-xone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both EndoMor-phins. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice.
Language
CLP2025 Biotin-Neurokinin B 神经