Opioid Receptor

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

Difelikefalin acetate (CR 845 acetate) is a peripherally restricted kappa opioid receptor agonist. CR845 exhibit low P450 CYP inhibition and low penetration into the brain.

DAMGO TFA (78123-71-4(Free base)) is a potent and selective agonist of the Mu-opioid receptor and an analgesic that stimulates calcium-activated adenylate cyclase-associated cAMP production and induces TGF-beta1 expression at the protein and mRNA levels.

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

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.

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

Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.

DAMGO (DAGO) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction.

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

LY2940094 (LY-2940094) decreases ethanol self-administration in animal models. LY2940094 is an effective, selective, and orally available nociceptin receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM).

CTAP(TFA) (103429-32-9 free base) is a potent, highly selective, and brain-penetrant antagonist of the μ-opioid receptor with IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP(TFA） (103429-32-9 free base) can be used for the study of L-DOPA-induced dyskinesia (LID)

SCH-486757 is an agonist of nociceptin-1 (NOP1) and orphanin FQ peptide receptors and is used in the study of cough.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2 iNOS expression.

Salvinorin A is a non-nitrogenous κ-opioid selective agonist.

Neuropeptide AF (human) acetate (Neuropeptide AF (human) acetate (192387-38-5 Free base)) is an anti-opioid neuropeptide, a Neuropeptide AF (human) derivative, which regulates adipocyte metabolism.

[Leu5]-Enkephalin (Leu-enkephalin) is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and μ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively)

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

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.

Dynorphin A acetate is an Endogenous kappa receptor agonist.

Sinomenine (Kukoline) is a pure alkaloid isolated from the Sinomenium acutum, is utilized in the treatment of rheumatism and arthritis.

Progesterone (Pregn-4-ene-3,20-dione) is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production.

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

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

PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

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 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

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

SCH 221510 is an orally available, selective and potent NOP agonist with an EC50 of 12 nM and a Ki of 0.3 nM.SCH 221510 has anxiolytic activity and can be used to study neurological disorders.

DPDPE TFA is selective δ-opioid receptor agonist peptide. Inhibits electrically stimulated contraction of mouse vas deferens in vitro (EC50 = 5.2 nM), and is antinociceptive in vivo.

Bevenopran (CB-5945) is a peripheral antagonist of μ-opioid receptor and can be used in studies about the treatment of opioid-induced bowel dysfunction.

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) is a potent agonist of the ORL1 KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.

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.

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

Nociceptin (1-13), amide is a potent agonist Opioid receptor-like1 (ORL1) receptor with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

Endomorphin 1 is a high affinity and selective agonist of the μ-opioid receptor and displays reasonable affinities for kappa3 binding sites (Ki: 20~30 nM).

Difelikefalin acetate (CR 845 acetate) is a peripherally restricted kappa opioid receptor agonist. CR845 exhibit low P450 CYP inhibition and low penetration into the brain.

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.

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

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 disorders, and may be used in the study of postherpetic neuralgia, knee osteoarthritis and pain.

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

1. Corydaline (Corydalin), an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent. 2. Corydaline promotes gastric emptying and small intestinal transit and facilitates gastric accommodation. 3. Corydaline exhibits the anti-acetylcholinesterase, antiallergic, and antinociceptive activities. 4. Corydaline has potent inhibition of CYP2C19 and CYP2C9.

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

(D-Ser2)-Leu-Enkephalin-Thr is a delta selective agent of opioid receptor and shows analgesic effects.

Nociceptin (1-7) acetate is a potent agonist of opioid receptor-like 1 (ORL1) receptor. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia and has antinociceptive activity.

Cerivastatin sodium (BAY W 6228 sodium) is an orally active and highly potent HMG-CoA reductase inhibitor with lipid-lowering activity that can reduce low-density lipoprotein cholesterol levels. Cerivastatin sodium has anticancer effects and can be used to study primary hyperlipidemia.

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.