Opioid Receptor

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

DPDPE is selective δ-opioid receptor agonist peptide.

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

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

MCOPPB triHydrochloride (MCOPPB 3HCl) is a nociceptin receptor agonist.

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

ADL-5747 (ADL-5747 (free base)) (free base) is a delta opioid receptor agonist used in the treatment of neurological disorders, skin and musculoskeletal

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

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

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

BW-180C (DADLE) is a prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1

EM-2 reduces sEPSC frequency/amplitude in lamina IX motoneurons; CTOP reverses this. EM-2-IR affects limb muscles via presynaptic/postsynaptic mechanisms.

Compound 46, designated as MOR agonist-2, serves as a D3R antagonist and a MOR agonist with respective K i values of 7.26 nM and 564 nM.

Asimadoline (EMD-61753) is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany.

Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM).

ICI 204,448 is a potent κ-opioid agonist with potential analgesic activity for the study of neurological diseases.

Opioid receptor agonist1 (Compound 2638-28) is an orally active opioid receptor agonist that shows strong affinity for MOR, DOR, and KOR, with Ki values of 5, 24, and 212 nM, respectively. It exhibits analgesic activity in both the mouse warm water tail-flick model and the acetic acid writhing model.

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,

6'-GNTI dihydrochloride is a κ-opioid receptor (KOR) agonist that favors activation of G-protein-mediated signaling over recruitment of β-aspirin 2.

IPAG is a potent σ-receptor antagonist (pKi=4.3). IPAG can induce cell apoptosis.

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.

Anilopam is an opioid analgesic belonging to the benzazepine class and acts as an agonist at opioid receptors.

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)

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.

LY2444296 (FP3FBZ) is an orally active and selective antagonist of kappa opioid receptor(Ki = 1 nM).

AH 8529 is an orally active opioid compound with analgesic properties.

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.

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

NNC 63-0532 is a potentnociceptin receptor agonist, Ki=7.3 nM, EC50=305 nM.

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

(-)-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.

EST73502 is an agonist of μ-opioid receptor(Ki = 64 nM) agonist and an antagonist of σ1 receptor (Ki = 118 nM). EST73502 displays antinociceptive activity.

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.

CP-866087 is a novel, potent and selective mu-opioid receptor antagonist for the study of female sexual dysfunction.

(R,S)-Ivosidenib is the less active enantiomer of Ivosidenib .

Propiram fumarate HClis an orally available Opioid receptors agonist with analgesic activity for the study of musculoskeletal pain.

BMS986187 is a novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Receptor.

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).

Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin), is a naturally occurring, endogenous opioid peptide that inhibits tumor growth via binding to the opioid receptor.

SCH 221510: oral NOP agonist, EC50=12 nM, Ki=0.3 nM, anxiolytic, for neurological research.

GSK1521498 is a selective antagonist of the μ-opioid receptor (MOR).

Opioid receptor modulator 1 is a modulator of opioid receptor.

BAN ORL 24 dihydrochloride is a highly potent nociceptin/orphan FQ (N/OFQ) receptor (NOP) antagonist that can be used to study neurological diseases.

R-6890 is an opioid compound with analgesic properties.

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

Dermorphin TFA is a new class of opioids-like peptides

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (

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).

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