Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. Opioid receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances. Opioid receptors inhibit the transmission of impulse in excitatory pathways within the human body system. These pathways include the serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being. Opioid receptors are further subclassified into mu, delta, and kappa receptors. All the classes, while exhibiting differing modes of action, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasma membrane of the majority of cells.


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Naltrindole hydrochloride

Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.

  • CAS Number: 111469-81-9
  • MF: C26H27ClN2O3
  • MW: 450.95700
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: 664.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 355.5ºC

Gluten Exorphin B5

Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats[1].

  • CAS Number: 68382-18-3
  • MF: C30H38N6O7
  • MW: 594.66
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

naltrexone

Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system[1].

  • CAS Number: 16590-41-3
  • MF: C20H23NO4
  • MW: 341.40
  • Catalog: Opioid Receptor
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 558.1±50.0 °C at 760 mmHg
  • Melting Point: 168-170ºC
  • Flash Point: 291.4±30.1 °C

BTRX-335140(CYM-53093

BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) [1].

  • CAS Number: 2244614-14-8
  • MF: C25H32FN5O2
  • MW: 453.55
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dermorphin TFA

Dermorphin TFA is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain[1].

  • CAS Number: 78331-26-7
  • MF: C42H51F3N8O12
  • MW: 916.89600
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAN ORL 24

BAN ORL 24 free base is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 free base has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 free base can be used for the research of cancer and analgesic[1].

  • CAS Number: 475150-69-7
  • MF: C27H35N3O2
  • MW: 433.59
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT-121

AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects[1].

  • CAS Number: 2099681-31-7
  • MF: C24H38N4O3S
  • MW: 462.65
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sec-O-Glucosylhamaudol

Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect[1].

  • CAS Number: 80681-44-3
  • MF: C21H26O10
  • MW: 438.425
  • Catalog: Opioid Receptor
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 677.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 237.2±25.0 °C

Naltriben mesylate

Naltriben mesylate is a potent delta-2 receptor-selective antagonist, with Kis are 0.013, 19 and 152 nM for δ, μ and κ receptors respectively. Naltriben mesylate selectively attenuates alcohol intake in rats bred for alcohol preference[1][2].

  • CAS Number: 122517-78-6
  • MF: C27H29NO7S
  • MW: 511.59
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

μ opioid receptor agonist 2

μ opioid receptor agonist 2 (Compound H-3)is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases[1].

  • CAS Number: 2671755-38-5
  • MF: C25H34N4O
  • MW: 406.56
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UFP-101 TFA

UFP-101 is a potent, selective, and competitive antagonist of the nociceptin/orphanin FQ (NOP) receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect[1][2].

  • CAS Number: 849024-68-6
  • MF: C82H138N32O21
  • MW: 1908.175
  • Catalog: Opioid Receptor
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dynorphin (2-17), amide (porcine)

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].

  • CAS Number: 161874-98-2
  • MF: C90H147N31O20
  • MW: 1983.33
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY-255582

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].

  • CAS Number: 119193-09-8
  • MF: C22H35NO2
  • MW: 345.51900
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GSK1521498

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].

  • CAS Number: 1426543-84-1
  • MF: C24H23F2N4O4P
  • MW: 500.43
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

U-69593

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].

  • CAS Number: 96744-75-1
  • MF: C22H32N2O2
  • MW: 356.50
  • Catalog: Opioid Receptor
  • Density: 1.14g/cm3
  • Boiling Point: 518.719ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 267.512ºC

Asimadoline

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.

  • CAS Number: 153205-46-0
  • MF: C27H30N2O2
  • MW: 414.539
  • Catalog: Opioid Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 605.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 320.2±31.5 °C

JDTic (dihydrochloride)

JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

  • CAS Number: 785835-79-2
  • MF: C28H41Cl2N3O3
  • MW: 538.54900
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 trifluoroacetate salt (Disulfide bond)

CTOP is a peptide that acts as a μ-opioid receptor antagonist.

  • CAS Number: 103429-31-8
  • MF: C50H67N11O11S2
  • MW: 1062.26000
  • Catalog: Opioid Receptor
  • Density: 1.42g/cm3
  • Boiling Point: 1491.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 855.7ºC

Trimebutine-d5

Trimebutine-d5 is the deuterium labeled Trimebutine. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects[1][2].

  • CAS Number: 1189928-38-8
  • MF: C22H24D5NO5
  • MW: 392.50000
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ADL5859 HCl

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.

  • CAS Number: 850173-95-4
  • MF: C24H29ClN2O3
  • MW: 428.952
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (Disulfide bond between Cys2 and Pen7)

CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID)[1].

  • CAS Number: 103429-32-9
  • MF: C51H69N13O11S2
  • MW: 1104.304
  • Catalog: Opioid Receptor
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
  • CAS Number: 59481-79-7
  • MF: C45H66N10O15S
  • MW: 1019.13000
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cebranopadol ((1α,4α)stereoisomer)

Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.

  • CAS Number: 863513-93-3
  • MF: C24H27FN2O
  • MW: 378.48
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DIPPA hydrochloride

DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant[1][2][3][4].

  • CAS Number: 155512-52-0
  • MF: C22H24Cl3N3OS
  • MW: 484.870
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

δ-Endorphin (human)

β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia[1][2].

  • CAS Number: 76622-84-9
  • MF: C139H217N33O40S
  • MW: 3022.47
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BMS-986188

BMS-986188 is a selective positive allosteric modulator of δ-opioid receptor with an EC50 of 0.05 μM[1].

  • CAS Number: 1776115-10-6
  • MF: C30H31BrO4
  • MW: 535.47
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZP 120C

ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia[1][3].

  • CAS Number: 383123-18-0
  • MF: C85HN27O15
  • MW: 1781.20
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ORL1 antagonist 1

ORL1 antagonist 1 is an opioid receptor-like 1 (ORL1) antagonist with an IC50 of 61 nM.

  • CAS Number: 1174985-59-1
  • MF: C20H22ClN5
  • MW: 367.88
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6β-Naltrexol

6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit[1].

  • CAS Number: 49625-89-0
  • MF: C20H25NO4
  • MW: 343.42
  • Catalog: Opioid Receptor
  • Density: 1.48g/cm3
  • Boiling Point: 557.5ºC at 760mmHg
  • Melting Point: 90-96ºC
  • Flash Point: 291ºC

Cebranopadol

Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.

  • CAS Number: 863513-91-1
  • MF: C24H27FN2O
  • MW: 378.482
  • Catalog: Opioid Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 547.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 284.9±30.1 °C