Opioid Receptor

<p>LY2940094 (LY-2940094) decreases ethanol self-administration in animal models.</p>

<p>Sinomenine hydrochloride (Kukoline hydrochloride) is extracted from Sinomenium Acutum Rehderett Wilson.</p>

<p>Apitegromab (SRK-015) is a new myostatin inhibitor, an antibody targeting myostatin precursor, which can be used to study neuromuscular diseases including</p>

<p>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.</p>

<p>Naltrexone hydrochloride (Naltrexone HCl) is a synthetic opioid antagonist used in the prevention of relapse of opiate addiction and alcoholism.</p>

<p>Meptazinol hydrochloride (Meptazinol HCl) , a unique centrally opioid analgesic, is used as a narcotic antagonist with analgesic properties.</p>

<p>BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity.Cost-effective and quality-assured.</p>

<p>Moguisteine (BBR-2173) is a new-type peripheral non-narcotic antitussive drug.</p>

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

<p>Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects.</p>

<p>Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.</p>

<p>Alvimopan is a potent opioid antagonist targeting gut receptors to reverse opioid effects on motility.</p>

<p>ZT 52656A is a selective agonist of kappa opioid, and used for the prevention or alleviation of pain in the eye.</p>

<p>CP 866087 is an opioid receptor antagonist for the study of female sexual dysfunction.</p>

<p>CSD-CH2(1,8)-NH2 is a selective and competitive kappa-opioid receptor (KOR) antagonist with a K i of 6.8 nM.</p>

<p>DPDPE is selective δ-opioid receptor agonist peptide.</p>

<p>Strong, selective NOP receptor antagonist with pKi=10.24; &gt;3000x selectivity over δ, μ, κ receptors; blocks nociceptin effects.</p>

<p>Dermorphin is agonist of μ-opioid receptor (MOR) agonist.</p>

<p>SNC 80, a non-peptide δ-opioid agonist (Ki=1.78 nM, IC50=2.73 nM), also targets μ-δ heteromers (EC50=52.8 nM), with analgesic and antidepressant potential.</p>

<p>[DPro10] Dynorphin A (1-11)acetate,porcine is a highly potent κ-opioid receptor agonist with a Ki value of 0.13 nM.</p>

<p>A unique collection of 1513 neurotransmitter receptor compounds, can be used for HTS and HCS screening；</p>

<p>DuP 747 HCl is a selective kappa agonist with analgesic activity.DuP 747 consists of two conformations.</p>

<p>β-Endorphin, equine TFA, an endogenous opioid peptide, demonstrates high affinity binding to μ/δ opioid receptors and possesses analgesic properties [1] [2] [3</p>

<p>Frakefamide TFA: potent, peripherally active μ-opioid agonist; doesn't cross blood-brain barrier.</p>

<p>4-Hydroxy-1-(2-phenylethyl)piperidine is a synthetic ligand for muscarinic acetylcholine receptors (mAChR) or non-opioid intracellular sigma-1 receptors (σ1 receptors). It serves as a metabolite of the opioid compounds furanylfentanyl and 4-fluoroisobutyryl fentanyl (FIBF).</p>

<p>U-48520 is an agonist of the μ-opioid receptor (μ-opioid receptor) with an EC50 of 1561 nM.</p>

<p>Selective δ opioid antagonist. Exhibits partial agonist in vitro activity at δ receptors at high concentrations.</p>

<p>DBPR116 is a prodrug of BPRMU191 that can penetrate the blood-brain barrier. It significantly enhances the delivery efficiency of drugs targeting the central nervous system. When combined with the antagonist Naltrexone, DBPR116 demonstrates superior safety and analgesic effects compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing promise as a safer opioid analgesic.</p>

<p>AH 7959 is an orally active N-substituted cyclohexylmethylbenzamide compound that exhibits analgesic properties. In mice, the ED50 for oral and subcutaneous administration of AH 7959 exceeds 100 mg/kg.</p>

<p>Biphalin TFA is an opioid peptide analog that penetrates the blood-brain barrier (BBB) and encompasses two active enkephalin pharmacophores.</p>

<p>NOP site high affinity ligand (Ki=1.5 nM); blocks nociceptin effects in rat brain/heart; agonist in vivo, reduces mouse movement.</p>

<p>Orphine is an opioid compound that can amplify the antinociceptive effects reduced by naloxone in mice.</p>

<p>AH 7563 is structurally classified as an opioid compound with analgesic properties. In mice, its ED50 for pain relief was 15.3 mg/kg when administered orally in the Phenylquinone test, and 15.5 mg/kg when injected subcutaneously in the Hot plate test.</p>

<p>Corynantheidine ((-)-Corynantheidine) is a partial agonist of the mu opioid receptor (MOR) and demonstrates MOR-dependent analgesic effects in mice.</p>

<p>Axelopran (TD-1211) treats opioid constipation; it's a potent, selective peripheral opioid blocker.</p>

<p>DAMGO is a selective peptide agonist of the µ-opioid receptor .</p>

<p>Fluorphine, an analog of Brorphine, binds to the μ-opioid receptor (MOR) with a Ki of 12.5 nM. It exhibits GTPγS binding activity with an EC50 of 75 nM and β-arrestin 2 recruitment activity with an EC50 of 377 nM, and it also has respiratory depressive effects.</p>

<p>KOR agonist 5 (Compound 10a) is both a KOR/MOR modulator, exhibiting agonistic effects on KOR and antagonistic effects on MOR. It effectively blocks morphine-induced antinociception and gastrointestinal motility inhibition. KOR agonist 5 is applicable in research related to substance use disorder (SUD).</p>

<p>HINT1-IN-1 (compound 8) is an inhibitor of histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. It influences the cross-regulation between μ-opioid receptors (MOR) and NMDA receptors (NMDAR).</p>

<p>KOR agonist 4 (compound 39) is an agonist targeting the κ opioid receptor (Kappa Opioid Receptor) and activates G protein signaling. It has an EC50 of 14 nM and an Emax of 83% for binding to GTPγS. This compound demonstrates moderate to high intrinsic clearance in human liver cells and shows selectivity for the κ opioid receptor over the μ (MOR) and δ (DOR) opioid receptors by factors of 60 and 810, respectively. KOR agonist 4 is useful for research into central nervous system (CNS) disorders.</p>

<p>Akuammicine, as an indole alkaloid from Catharanthus roseus, can be used in cancer cell eradication.</p>

<p>Bioactive metabolite of nociceptin, antagonist of nociceptin-induced hyperalgesia</p>

<p>Potent, selective OP4 agonist; pKi=10.68, pEC50=9.80. &gt;8000x selectivity vs other opioid receptors; long-lasting in vivo effects.</p>

<p>Dermorphin Analog, a heptapeptide from amphibian skin, binds μ-opioid receptors selectively and strongly.</p>

<p>KOR agonist 3 (Compound 5) is an agonist of the κ opioid receptor (κOR) with an EC50 of 0.88 nM. It also exhibits some activation of μOR, with an EC50 of 720 nM. However, KOR agonist 3 does not activate δOR at concentrations below 1 μM. Its ability to recruit β-Arrestin-2 is lower than that of U50488.</p>

<p>μ opioid receptor agonist; IC50: 5.5 nM (μ), &gt;10,000 nM (δ). Induces reversible analgesia, catalepsy, hyperthermia in rats.</p>

<p>(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine) is a demethylated analog of Mitragynine, functioning as a selective and partial agonist for the μ-opioid receptor (μ-opioid receptor). This compound inhibits electrically stimulated twitch contractions in the guinea pig ileum.</p>

<p>Ro 64-6198: Nonpeptide, selective NOP agonist, high brain uptake, EC50=25.6 nM, 100x NOP&gt;opioid affinity.</p>

<p>Nociceptin peptide fragment (1-11) with potent ORL1/KOR-3 receptor agonism (Ki = 55 nM), no opioid receptor affinity, and analgesic in mice.</p>

<p>Piperidylthiambutene hydrochloride is an opioid compound that exhibits analgesic effects in animal models.</p>

<p>Competitive nociceptin receptor antagonist with pKi=8.4; no agonist activity; blocks nociceptin effects in vitro/in vivo.</p>

<p>U-54494A hydrochloride is a benzamide derivative related to kappa opioid receptor agonists. U-54494A hydrochloride has anticonvulsant activity.</p>

<p>AH 8529 is an orally active opioid compound with analgesic properties.</p>

<p>Gluten exorphin B5 (GE-B5) is a food-derived opioid peptide identified in digests of wheat gluten.</p>

<p>Herkinorin: μ-opioid agonist with 100x μ-affinity, 50x less κ-affinity than Salvinorin A, from Salvia divinorum. Semi-synthetic from Salvinorin B.</p>

<p>AH 8532 is an opioid compound with analgesic effects and is effective in inhibiting the quinone-induced writhing response in mice, with an oral ED50 of 16 mg/kg.</p>

<p>Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.</p>

<p>Neuropeptide AF (93-110), Human is an endogenous antiopioid peptide.</p>

<p>Potent μ opioid antagonist, IC50 3.5 nM, 1200x selectivity over δ and somatostatin, brain-penetrant, active in vivo.</p>

<p>R-6890 is an opioid compound with analgesic properties.</p>

<p>β-Naltrexamine dihydrochloride is an orally administered, irreversible opioid receptor antagonist. Its derivatives exhibit optimised subtype selectivity and can be used for pain research.</p>

<p>N-Phenethylnoroxymorphone is an opioid compound that can enhance morphine-induced analgesia in rats. It is used in the research of neurological disorders.</p>

<p>Potent μ-receptor antagonist, Ki=0.96nM, ineffective at δ (&gt;10,000nM). Alters behavior in vivo, boosts K+ currents in rat neurons in vitro, μ-independent.</p>

<p>Cebranopadol hemicitrate is a NOP and opioid receptor agonist that targets human NOP, MOP, KOP, and δ-opioid peptide (DOP) receptors, with Ki/EC50 values of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, and 18 nM/110 nM, respectively. It is used in studies of acute and chronic pain.</p>

<p>AP-238 is a novel synthetic opioid (NSO) that acts as an agonist for the μ-opioid receptor (MOR), with an EC50 of 248 nM. Additionally, AP-238 exhibits analgesic properties.</p>

<p>MT-7716: selective NOP agonist, potential in preventing alcohol abuse/relapse.</p>

<p>LY255582 is a selective centrally active opioid receptor antagonist with high affinity for mu, delta and kappa receptors with Ki of 0.4 nM, 5.2, 2.0 nM,</p>

<p>Bovine adrenal medulla docosapeptide (BAM-22P) is a potent opioid agonist, derived from the proenkephalin A gene, which is present in the adrenal medulla.</p>

<p>TAN67 is the first effective selective non-peptide delta1 opioid receptor.</p>

<p>Boc-ypgflt(O-tbu) is a delta-receptor-selective opioid antagonist.</p>

<p>Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid</p>

<p>(Rac)-SNC80, a racemic δ-opioid agonist (K i 1.78 nM), shows potential for treating various headache disorders.</p>

<p>Selective NOP receptor partial agonist peptide; Ki=0.71 nM; &gt;4000 nM for μ, δ, κ receptors; boosts food intake in vivo.</p>

<p>Naldemedine (S 297995), developed by Shionogi, is a drug for opioid side effects like constipation. It's well tolerated with minor GI issues.</p>

<p>AT-121 hydrochloride: dual nociception/mu-opioid agonist, Ki 3.67/16.49 nM, safe, non-addictive pain reliever with analgesic effects.</p>

<p>Potent NOP agonist (EC50 = 1 nM), &gt;875x selective vs opioid receptors; outperforms nociceptin in vivo, increases pain perception, reduces movement.</p>

<p>N-Desmethyl Loperamide is the major metabolite of loperamide. It is also used as the precusor for radiolabelled loperamide.</p>

<p>Endorphin Beta is A substance produced in the brain, especially in the pituitary gland, Endorphin Beta blocks the sensation of pain.</p>

<p>MT-7716 hydrochloride is a selective agonist of non-peptide nociceptin receptor (NOP)</p>

<p>(S,S)-J-113397 is an isomer of J-113397 . J-113397 is an Opioid Receptor antagonist [1] .</p>

<p>Clocinnamox mesylate: irreversible μ-opioid blocker; Ki: 0.7 nM (mouse μ), 1.9 nM (δ), 5.7 nM (κ).</p>

<p>Adrenorphin (Metorphamide)(3TFA) is an agonist of μ-opioid receptor(Ki :12 nM).</p>

<p>[Met5]-Enkephalin, amide activates δ and ζ opioid receptors; has multiple forms and varying plasma levels.</p>

<p>Valorphin (Valorphin TFAsalt) has opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM.</p>

<p>E-2078, known chemically as (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8), is a stable analog of Dynorphin A (1–8) and functions as a kappa opioid</p>

<p>[Nphe1]Nociceptin(1-13)NH2 is a selective nociceptin receptor antagonist with potential analgesic properties, pKi=8.4, pA2=6.0.</p>

<p>Nocistatin, a neuropeptide, blocks Nociceptin effects and inhibits 5-HT release, acting on an opioid-related receptor.</p>

<p>Helianorphin-19: Potent KOR agonist (Ki=25 nM; EC50=45 nM), 200x selective over μ/δ receptors, effective in mouse pain model, non-sedative.</p>

<p>β-Lipotropin (60-65) (β-LPH (60-65)), an opioid agonist, is a significant [1] opioid peptide.</p>

<p>'[DAla2, DArg6] Dynorphin A (1-13) porcine is a potent opioid peptide resistant to enzymatic degradation.'</p>

<p>β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities.</p>

<p>Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor .</p>

<p>Ac-RYYRWK-NH2: potent, specific NOP receptor partial agonist with 0.071 nM affinity; no affinity for μ/κ/δ-opioid receptors.</p>

<p>Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain</p>

<p>BPR1M97 is a mu opioid receptor (MOP) and neuropeptide-orphin FQ (NOP) receptor agonist with blood-brain barrier permeability and potency, with Kis values of 1.</p>

<p>PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist that activates the G protein signaling pathway with an EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). Additionally, PIPE-3297 promotes myelination and has anti-inflammatory properties.</p>

<p>β-Endorphin (1-27) (human) is an opioid antagonist that selectively binds to μ-, δ-, and κ-opioid receptors, with dissociation constants (Kis) of 5.31, 6.17,</p>

<p>non-peptide δ1 opioid receptor agonist</p>

<p>Dynorphin B (1-9), a neuropeptide and the N-terminal cleavage product of dynorphin B, has its formation inhibited by N-ethylmaleimide (NEM), a non-selective</p>

<p>DALDA TFA is a potent, μ-opioid receptor agonist exhibiting high selectivity and an affinity constant (K i) of 1.69 nM.</p>

<p>Leumorphin, human, is a potent agonist of the kappa opioid receptor (κ opioid receptor) and inhibits the contraction of the guinea pig ileum's myenteric plexus-</p>

<p>Deltorphin acetate is a substance obtained from the skin secretions of a frog, Phyllomedusa bicolor and shows high selectivity and affinity for δ-opioid</p>

<p>CJ-15208: κ-opioid antagonist, IC50: 47 nM kappa, 260 nM mu, 2600 nM delta, reverses asimadoline effects in rabbits (ED50 1.3 µM).</p>

<p>N-terminally acetylated Endomorphin-1 is a modified Endomorphin-1.</p>