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HS666 hydrochloride
- Parent CAS: 1409931-91-4
- Soluble in DMSO
- MF: C20H25NO.HCl
- MW: 331.88
Description
HS666 hydrochloride is a selective partial agonist of the κ-opioid receptor (KOR/OPRK1) with a Ki value of 5.9 nM. It activates G-protein-mediated KOR signaling while displaying relatively low efficacy for β-arrestin-2 recruitment.
HS666 produces KOR-dependent antinociceptive effects in preclinical models and has been used to investigate whether reduced β-arrestin signaling can separate analgesic-like responses from aversive or dysphoric effects. It is a useful ligand for pathway-bias, receptor-efficacy and opioid-behavior studies.
Key Features
- High-affinity KOR partial agonist
- Ki: 5.9 nM
- Low β-arrestin-2 signaling efficacy
- Produces central KOR-dependent antinociception
Applications
- κ-Opioid receptor pharmacology
- Biased-agonism studies
- G-protein versus β-arrestin signaling
- Pain and antinociception models
- Aversion and reward-behavior research
More Information
| Parent CAS No. | 1409931-91-4 |
|---|---|
| Chemical Name | 3-(2-((Cyclopropylmethyl)(phenethyl)amino)ethyl)phenol hydrochloride |
| SMILES | C1(O)C=C(CCN(CC2CC2)CCC2C=CC=CC=2)C=CC=1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C20H25NO.ClH/c22-20-8-4-7-18(15-20)12-14-21(16-19-9-10-19)13-11-17-5-2-1-3-6-17;/h1-8,15,19,22H,9-14,16H2;1H |
| InChiKey | COAVTAYHWOYAEJ-UHFFFAOYSA-N |
| CID | 71513817 |
| Short Description | Kappa-opioid partial agonist |
References
- M Spetea et al. Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. J Med Chem. 2012 Nov 26;55(22):10302-6.
- M Spetea et al. Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice. Br J Pharmacol. 2017 Aug;174(15):2444-2456.
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