ADL5859

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

ADL5859 是一种有效、选择性、口服生物可利用的 δ 阿片受体完全激动剂，Ki 为 0.84 nM，EC50 为 20 nM。

ADL5859 is a potent, selective, orally bioavailable full agonist of δ opioid receptor with Ki of 0.84 nM and EC50 of 20 nM, exhibits >1,000-fold selectivity for δ over μ and κ opioid receptors in both receptor binding and in vitro bioassays; demonstrates analgesic and antidepressive effects in the rat and represent potential drug for chronic pain treatment, significantly reduces inflammatory and neuropathic pain, does not induce either hyperlocomotion or receptor internalization in vivo.Pain Phase 2 Discontinued.

ADL-5859 (0-10 μM) hydrochloride shows activities to δ opioid receptor with an Ki and an EC50 value of 0.84 and 20 nM, and inhibits 32% and 37% activities to μ 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.

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.Animal Model:Rats with Freund’s Complete Adjuvant (FCA) injection induced mechanical hyperalgesia Dosage:0.3-10 mg/kg Administration:Oral gavage; 0.3-10 mg/kg once Result:Produced 100% reversal of hyperalgesia in the inflamed paw with a dose of 3 mg/kg and showed an oral ED50 value of 1.4 mg/kg.Animal Model:Male Sprague-Dawley rats Dosage:0.3 and 3 mg/kg Administration:Oral gavage; 0.3 and 3 mg/kg once Result:Produced robust antidepressant-like activity in the rat forced swim assay with a dose of 3 mg/kg.

ADL-5859 | ADL 5859

Endocrinology/Hormones

Opioid Receptor

δ-opioidreceptor|κ-opioidreceptor|μ-opioidreceptor

Neurological Disease

Pain

850173-95-4

428.9517

C24H29ClN2O3

>98% (HPLC)

10 mM in DMSO

CCN(CC)C(=O)C1=CC=C(C=C1)C2=CC3(CCNCC3)OC4=CC=CC(=C42)O.Cl

Benzamide, N,N-diethyl-4-(5-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-4-yl)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years