Opioid Receptor

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor, derived from patent WO2014107344. BMS-986121 is built on a chemical scaffold and represents a new chemical type of μ receptor PAMs.

KNT-127 is an effective selective δ opioid receptor agonist that works effectively through systemic administration. KNT-127 has selectivity for the δ receptor (with Ki values of 21.3, 0.16, and 153 nM for opioid receptors μ, δ, and κ, respectively). It can increase dopamine and L-glutamate release in the striatum, ventral pallidum, and anterior cingulate cortex. It also exhibits antidepressant-like effects.

(Rac)-SNC80 is the racemic form of SNC80. SNC80 (NIH 10815) is an effective and highly selective non-peptide delta-opioid receptor agonist with a Ki of 1.78 nM and IC50 of 2.73 nM. SNC80 has anti-nociceptive, anti-hyperalgesic, and antidepressant-like effects, and can be used in research on various types of headaches.

(1R,2R)-U-50488 hydrochloride is the absolute configuration of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a κ opioid receptor agonist.

TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM.

MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.

J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.

LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively).

Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors.

Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA).

β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors.

DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM.

Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors.

TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist ( K D = 70 nM) with blood-brain barrier permeability.

Sialorphin TFA is a neutral endopeptidase ( NEP ) and aminopeptidase N ( APN ) inhibitor that responds to androgen signals.

RB 101 hydrochloride is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor.

Sinomenine Hydrochloride is an inhibitor of NF-κB activation.

b-Casomorphin (1-3), with the sequence H2N-Tyr-Pro-Phe-OH, is an opioid-like active tripeptide obtained from the enzymatic digestion of bovine β-casein.

δ receptor antagonist

Endomorphin-2 is a high-affinity and highly selective agonist of the μ-opioid receptor (K i = 0.69nM).

DPDPE is a selective and anticonvulsant δ-opioid receptor (DOR) agonist.