κ-opioid receptor

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

Muopioid Receptor Antagonist 8 (368) serves as an antagonist to the μ-opioid receptor, significantly inhibiting the activation of Gi induced by met-enkephalin at the µOR.

Opioid receptor modulator 1 is a modulator of the opioid receptor.

μ opioid receptor agonist 2 (Compound H-3) is a MOR receptor agonist used for research on pain and pain-related diseases.

σ 1 Receptor/ μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

Compound 12, a Mu-opioid receptor agonist, activates Mu-opioid receptors. It is utilized in research related to the nervous system.

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM), and can be used to study opioid use disorder (OUD).

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (IC50) of 29 ± 3.0 nM. It is valuable for pain and opioid use disorder research [1].

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective MOR antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM) and can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier, with an EC50 of 1.14 nM and a Ki of 0.37 nM. Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

μ opioid receptor agonist 1 (Compound H-1a) is an optically pure oxyheterocyclic substituted pyrroloxypyrazole derivative and an MOR receptor agonist that can be used in the study of pain and pain-related disorders.

BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity against κOR, μOR, and δOR with IC50 values of 0.8, 110, and 6500 nM, respectively.

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

Matrine (Vegard), an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.

Dynorphin A (1-10) acetate is 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.

[DPro10] Dynorphin A (1-11)acetate,porcine is a highly potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine is an n-alkylated derivative with analgesic activity.

Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.

6'-GNTI dihydrochloride is a κ-opioid receptor (KOR) agonist that favors activation of G-protein-mediated signaling over recruitment of β-aspirin 2. 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.

beta-Neoendorphin acetate is an agonist of κ-opioid receptor

Porcine dynorphin A(1-13) acetate (Dynorphin A Porcine Fragment 1-13 acetate) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons similar to increases seen with acute NMDA treatment.

[(pF)Phe4]Nociceptin(1-13)NH2 acetate is a selective agonist of NOP receptor with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 acetate displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

GR103545 is a selective agonist of the κ-opioid receptor, which is a radiotracer that can be used as in vivo imaging.

UFP-101 acetate is a selective and competitive antagonist of the NOP receptor (pKi = 10.24) with >3000-fold selectivity over δ, μ, and κ opioid receptors.

Norbinaltorphimine dihydrochloride is a selective and potent κ opioid receptor antagonist that induces itch-associated responses in mice.

ICI 199,441 hydrochloride is a potent, selective agonist of κ-opioid receptor.

ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.

LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

Cebranopadol (GRT6005) is an analgesic NOP and opioid receptor agonist with Kis of 0.9 nM, 0.7 nM, 2.6 nM, 18 nM for human NOP, μ-opioid (MOP), κ-opioid (KOP) and δ-opioid (DOP) receptor, respectively.

Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In vivoHelianorphin-19 shows potent peripheral analgesic efficacy in a mouse model of visceral pain without affecting motor coordination/sedation.

Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.

Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg/animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)

Riminkefon is a kappa opioid receptor agonist.

4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors, respectively. Calculated logBB and CNS (central nervous system) multiparameter optimization (MPO) and low molecular weight values all predict that 4-Me-PDTic will penetrate the brain and pharmacokinetic studies in rats shows that 4-Me-PDTic does indeed penetrate the brain.

Naldemedine tosylate (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) with high binding affinities (K_i = 0.34, 0.43, 0.94 nM) and potent antagonist activities (IC_50 = 25.57, 7.09, 16.1 nM) towards human recombinant μ-, δ-, and κ-opioid receptors, respectively. It is utilized in research on opioid-induced constipation (OIC) and is anticipated to interact with the 3CL proenzyme encoded by the SARS-CoV-2 genome.

Porcine dynorphin A (1-13), a potent endogenous κ opioid receptor agonist, exhibits antinociceptive properties at physiological concentrations and induces acute increases in [Ca2+]i in neurons, akin to those observed with acute NMDA treatment.

Dinalbuphine sebacate is a long-lasting prodrug of nalbuphine, acting as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor and as a high-efficacy partial agonist of the κ-opioid receptor.

Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.

Dynorphin B (1-13) TFA, an agonist of the opioid κ-receptor.

Dynorphin B (1-13) acts as an agonist on the opioid κ-receptor.

ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverses loperamide-induced delayed gastric emptying in a rat model of castor oil-induced diarrhea.

CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502 (IC50 are 47 nM for kappa, 260 nM for mu, and 2,600 nM for delta respectly). In the electrically-stimulated twitch response assay of rabbit vas de

Potent, selective partial agonist peptide for the NOP receptor (Ki = 0.71 nM). Selective over μ, δ and κ opioid receptors (IC50 > 4000 nM). Increases food intake in vivo.

Highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80). Displays > 8000-fold selectivity over δ, κ, and μ opioid receptors and has relatively long lasting pronociceptive, hypotensive, negative inotrop

NOP receptor antagonist

Difelikefalin HCl is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin HCl is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).

Bucinnazine is a potent and selective agonist of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor.