For research use only. Not for therapeutic Use.
HS666 is a selective κ opioid receptor partial agonist (Ki value of 5.9 nM) which activates central κ receptors to produce potent antinociception. Moreover, HS666 displays pharmacological characteristics of a κ receptor analgesic with reduced liability for aversive effects correlating with its low efficacy in the β-arrestin2 signalling pathway.
Keywords: HS666 hydrochloride | supplier | Kappa-opioid partial agonist | HS 666 hydrochloride | HS-666 hydrochloride | CAS [1409931-99-2] | [1409931-91-4] | Opioids | OPR-κ | Partial agonist | Receptors | Antinociception
Catalog Number | I047626 |
CAS Number | 1409931-99-2 |
Molecular Formula | C20H25NO.HCl |
Purity | ≥95% |
IUPAC Name | 3-[2-[cyclopropylmethyl(2-phenylethyl)amino]ethyl]phenol;hydrochloride |
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 |
SMILES | C1CC1CN(CCC2=CC=CC=C2)CCC3=CC(=CC=C3)O.Cl |
Reference | 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. |