产品
编 号：F155473
分子式：C32H37N5O5
分子量：571.67
分子式：C32H37N5O5
分子量：571.67
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CAS No: 141801-26-5
产品详情
生物活性：
Endomorphin 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.
体内研究：
Both Endomorphin 1 and Endomorphin 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. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice.
体外研究：
Endomorphin 2 is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 1 (EM-2). The two Endomorphins display reasonable affinities for kappa3 binding sites, with Ki values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ1 and μ2 receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa1 binding sites, with Ki values greater than 500 nM.
Endomorphin 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.
体内研究：
Both Endomorphin 1 and Endomorphin 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. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice.
体外研究：
Endomorphin 2 is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 1 (EM-2). The two Endomorphins display reasonable affinities for kappa3 binding sites, with Ki values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ1 and μ2 receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa1 binding sites, with Ki values greater than 500 nM.
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