LY2444296

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

LY2444296 是一种有口服生物活性、高亲和力、选择性的短效的 KOPR 拮抗剂，其 Ki 值为 ~1 nM。LY2444296 具有抗焦虑样的作用。

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ～1 nM. LY2444296 exhibits anti-anxiety like effects.

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LY2444296 displays anti-anxiety like effects in the EPM test.LY2444296 (3 mg/kg; i.p.; 30 min before U69,593 administration) prevents behavioral and neuroendocrine effects caused by the reference kappa agonist U69,593 in cocaine-na?ve rats.LY2444296 reduces anxiety-like and depressive-like behaviors, as well as CORT release, in rats tested after chronic extended access cocaine self-administration, but not in cocaine-na?ve rats.Animal Model:Adult male Sprague Dawley rats (240–250 g)Dosage:3 mg/kg Administration:Injected intraperitoneally; 30 min before U69,593 administration Result:Prevented behavioral and neuroendocrine effects caused by U69,593 in cocaine-na?ve rats.

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Endocrinology/Hormones

Opioid Receptor

Opioid Receptor

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1346133-11-6

408.44

C24H22F2N2O2

>98% (HPLC)

In Vitro:?Ethanol 中的溶解度 : 27.5 mg/mL (67.33 mM; 超声助溶)

NC(=O)c1ccc(Oc2ccc(CN3CCC[C@H]3c3cccc(F)c3)cc2)c(F)c1

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(-20℃)

With Ice Pack

≥ 2 years