ADL5859

SKU: orb1223860

Description

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.

Key Properties

• CAS Number: 850173-95-4
• MW: 428.9517
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₉ClN₂O₃
• SMILES: CCN(CC)C(=O)C1=CC=C(C=C1)C2=CC3(CCNCC3)OC4=CC=CC(=C42)O.Cl
• Target: Opioid Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• 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. 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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ADL-5859 | ADL 5859

Quick Database Links

Gene Symbol

Opioid Receptor