Enadoline

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Enadoline (CI 977;PD 129290) 是一种有效的选择性 κ-阿片受体 (KOR) 激动剂，Ki 为 0.11 nM。

Enadoline (CI 977;PD 129290) is a potent, selective κ-opioid receptor (KOR) agonist with Ki of 0.11 nM, binding with high affinity to [3H]-U69593-labelled kappa-sites; produces a potent inhibition of the electrically-evoked contractions of the guinea-pig ileum and rabbit vas deferens with IC50 values of 0.087 nM and 3.3 nM, respectively; is effective in reducing infarction in a model of focal cerebral ischaemia.Pain Phase 2 Discontinued.

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Enadoline (i.v.; dose of e 15 min before surgery; male Sprague-Dawley rats) dose-dependently (1-100 μg/kg) blocks the development of thermal hyperalgesia as well as static and dynamic allodynia for over 24 h with respective MEDs (minimum effective doses) of < or = 1, 10 and 10 μg/kg.

CI 977 | PD 129290

Endocrinology/Hormones

Opioid Receptor

Opioid Receptor

Neurological Disease

Pain

124378-77-4

396.531

C24H32N2O3

>98% (HPLC)

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CN(C1CCC2(CCCO2)CC1N3CCCC3)C(=O)CC4=C5C=COC5=CC=C4

2-(1-benzofuran-4-yl)-N-methyl-N-[(5R,7S,8S)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide

(-20℃)

With Ice Pack

≥ 2 years