Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect[1].
CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID)[1].
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice[1][2].
A potent and selective δ-opioid receptor agonist that has high affinity and selectivity for the δ1 subtype with Ki of 1.12 nM; dispalys >1,000-fold selectivity over μOR and κOR; Pain Discontinued
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment[2].
BAN ORL 24 is a potent and selective NOP receptor antagonist. (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively). IC50 value: 0.27 nMTarget: NOP receptorBAN ORL 24 inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca2+ mobilization in CHO cells in vitro. BAN ORL 24 antagonizes NOP agonist-induced reduction in locomotor activity in vivo. Brain penetrant.
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3].
μ opioid receptor agonist 1 （Compound H-1a）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases[1].
SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys[1][2].
CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure[1].
LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]Target: κ-opioid Receptorin vitro: LY2795050 displays full antagonist activity and high binding affinity and selectivity for KOR with a ki value of 0.72 nM [1].in vivo: In the brain, (11)C-LY2795050 displayed fast uptake kinetics (regional activity peak times of <20 min) and an uptake pattern consistent with the distribution of KOR in primates [1]. The LY2795050 ED50 at MOR was 119 μg/kg based on a 1-site model for 11C-carfentanil. The 1-site binding model was also deemed sufficient to describe the specific binding of 11C-LY2795050 at KOR. The ED50 at KOR estimated from the 1-site model was 15.6 μg/kg. Thus, the ED50 ratio for MOR:KOR was 7.6 [2].
β-Lipotropin (61-69) is a potent opioid agonist[1][2].
Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system[1][2].
NNC63-0532 is a novel non-peptide nociceptin receptor (ORL1) agonist, with EC50s of 305?nM. NNC63-0532 plays important roles in many disorders such as pain, drug addiction[1].
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ[1].
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant[1][2][3][4].
Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR[1].
β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia[1][2].
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP (OP4) agonists, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold)[1][2].
BMS-986188 is a selective positive allosteric modulator of δ-opioid receptor with an EC50 of 0.05 μM[1].
ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion[1].
ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia[1][3].
ORL1 antagonist 1 is an opioid receptor-like 1 (ORL1) antagonist with an IC50 of 61 nM.
Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1)[1].
6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit[1].
Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property[1][2].