Naltrexone-d4 is deuterium labeled Naltrexone.
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively[1].
Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia[1].
Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation[1].
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia[1].
Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
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). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity[1][2][3][4].
CYT-1010 is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively[1].
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs[1].
μ opioid receptor agonist 3 (compound 20) is a potent μ opioid receptor (µOR) agonist with an EC50 of 0.87 nM. μ opioid receptor agonist 3 has the potential for pain and neuropsychiatric indications research[1].
U-69593 is a potent and selective κ1-opioid receptor agonist[1]. U-69593 attenuates cocaine-induced behavioral sensitization in the rat[2]. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice[3]. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum[4].
Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM)[1][2].
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors[1].
Methylnaltrexone D3 Bromide is the deuterium labeled Methylnaltrexone Bromide. Methylnaltrexone Bromide is a peripheral-acting opioid receptor antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.
Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease[1][2].
Deltorphin 2 is a selective peptide agonit for the δ opioid receptor.
Herkinorin is a potent and selective agonist of µ opioid receptor with a Ki of 45 nM Herkinorin is widely used for pain research[1].
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs[1][2][3].
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction[1][2].
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects.Target: Opioid ReceptorTrimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain [1]. The major product from drug metabolism of trimebutine in human beings is nor-trimebutine, which comes from removal of one of the methyl groups attached to nitrogen. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract [2, 3].
CTOP is a peptide that acts as a μ-opioid receptor antagonist.
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR)[1].
Trimebutine-d5 is the deuterium labeled Trimebutine. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects[1][2].
ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. IC50 value: 0.8 nM(Ki)Target: δ-opioid receptorADL-5859 (ADL5859) is an δ-opioid receptor agonist (Ki=0.84 nM, EC50=20 nM). ADL-5859 (ADL5859) is an agonist agent that selectively stimulates the δ-opioid receptor with potential application in a wide range of inflammatory, neuropathic and acute pain conditions. In addition, Delta agonists are thought to modulate other biological processes that may manifest themselves in disease states or conditions such as overactive bladder and depression.ADL-5859 (ADL5859) is useful for inflammatory, neuropathic and acute pain conditions.
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain[1].
ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
Loperamide phenyl is an impurity of Loperamide (HY-B0418A). Loperamide is an opioid receptor agonist[1].