产品
编 号:F763060
分子式:C36H42N6O7
分子量:670.75
产品类型
结构图
CAS No: 1276123-71-7
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产品详情
生物活性:
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties.
体内研究:
Endomorphin 1 (i.c.v.) acetate shows antinociceptive properties in mice, with an ED50 value of 6.16 nM.Endomorphin 1 (50 μg/kg, i.v., rats) acetate alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response.Animal Model:ICR mice.
Dosage:6.16 nM (ED50)
Administration:Intracerebroventricularly (i.c.v.) injection
Result:Inhibited dose-dependently the tail-flick response.
Animal Model:Rats.
Dosage:50 μg/kg
Administration:Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min.
Result:Alleviated MIRI by reducing the production of free radicals.Dncreased LDH and CK-MB activities.Increased SOD activity and decreased MDA content.Decreased IL-6 and TNF-α plasma content.
体外研究:
Endomorphin 1 acetate 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) acetate increases interleukin-8 secretion in Caco-2 cells.Endomorphin 1 (1 μM) acetate inhibits excitatory transmission in adult rat substantia gelatinosa neurons.