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ADL-5859 hydrochloride

CAS No. : 850173-95-4

MCE 站：ADL-5859 hydrochloride

产品活性：ADL-5859 hydrochloride (compound 20) 是选择性的、具有口服活性的 δ opioid receptor (DOR) 激动剂，K_i 值为 0.84 nM，EC₅₀ 值为 20 nM。ADL-5859 hydrochloride 对 hERG 具有抑制活性，IC₅₀ 值为 78 μM。ADL-5859 hydrochloride 可用于痛觉的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease

作用靶点：Opioid Receptor  |  Potassium Channel  |  Cytochrome P450

In Vitro: ADL-5859 (0-10 μM) hydrochloride shows activities to δ opioid receptor with an K_i ａnd an EC₅₀ value of 0.84 ａnd 20 nM, ａnd inhibits 32% ａnd 37% activities to ａnd κ opioid receptor, respectively.
ADL-5859 (0-100 μM) hydrochloride exhibits inhibitory activity to hERG channel with an IC₅₀ value of 78 μM.
ADL-5859 (0-100 μM) hydrochloride inhibits activity of the drug metabolizing enzyme cytochrome P450 2D6 (CYP2D6) in vitro with an IC₅₀ value of 43 μM.

In Vivo: ADL-5859 (0.3-10 mg/kg; p.o. once) hydrochloride reverses hyperalgesia in inflamed paw of rats ａnd shows robust antidepressant-like activity.
Pharmacokinetic Properties of ADL-5859 in Rats ａnd Dogs.

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