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Endocrinology/Hormones Opioid Receptor

Opioid Receptor

Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin receptors (SSTRs). Opioid receptors are distributed widely in the brain, in the spinal cord, on peripheral neurons, and digestive tract.
Cat No. product name
T0102 Naloxone hydrochloride Naloxone hydrochloride is a specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
T0137 Mirtazapine Mirtazapine is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevat...
T0201 Meptazinol hydrochloride Meptazinol Hcl, a unique centrally opioid analgesic, is used as a narcotic antagonist with analgesic properties.
T0209 Loperamide hydrochloride Loperamide Hydrochloride is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.
T0262 Dextromethorphan HBr monohydrate Methyl analog of DEXTRORPHAN that shows high-affinity binding to some areas of the brain, including the medullary cough center. This compound is an NMDA recepto...
T0478 Progesterone Progesterone is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY ...
T0783 Mianserin hydrochloride Mianserin hydrochloride is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin ...
T0918 Trimebutine Trimebutine is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid agonist eff...
T0929 Docusate sodium Docusate is an orally available, over-the-counter laxative and stool softener used to treat or prevent constipation. Docusate has not been linked to serum enzym...
T0963 Naltrexone hydrochloride Naltrexone is a synthetic opioid antagonist used in the prevention of relapse of opiate addiction and alcoholism.
T0981 Noscapine hydrochloride Noscapine Hydrochloride is the orally available hydrochloride salt of the opioid agonist noscapine, a phthalide isoquinoline alkaloid derived from the opium pop...
T11198 Endomorphin 2 TFA Endomorphin 2 TFA,  displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. a high affinity, highly selective agonist of ...
T11478 GSK1521498 free base (hydrochloride) GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. GSK1521498 free base (...
T11478L GSK1521498 free base GSK1521498 free base is a potent and selective antagonist of μ-opioid receptor. GSK1521498 free base also has the potential for disorders of compulsive consump...
T11479 GSK1521498 GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and drugs. GSK1521498 is a potent and selective μ-opioid receptor (MOR)...
T12168 Naloxone benzoylhydrazone Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opio...
T12169 Naltrindole hydrochloride Naltrindole hydrochloride is a highly potent and selective antagonist of non-peptide δ opioid receptor(Ki of 0.02 nM).
T12241 Norbinaltorphimine dihydrochloride Norbinaltorphimine dihydrochloride is a potent and selective antagonist of κ opioid receptor.
T12314 Opioid receptor modulator 1 Opioid receptor modulator 1 is a modulator of opioid receptor.
T1242 Alvimopan Alvimopan is a synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a se...
T13419 ROCK-IN-1 ROCK-IN-1 is a potent ROCK inhibitor(IC50 of 1.2 nM , ROCK2).
T13438 (R,S)-Ivosidenib (R,S)-Ivosidenib is the less active enantiomer of Ivosidenib .
T1407 L-Menthol L-Menthol is a levo isomer of menthol, an organic compound made synthetically or obtained from peppermint or mint oils with flavoring and local anesthetic prope...
T14551 Bevenopran Bevenopran is an antagonist of peripheral μ-opioid receptor.
T15165 DPI-3290 DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinoci...
T2071 MCOPPB trihydrochlride MCOPPB trihydrochlride is a nociceptin receptor agonist.
T2388 Nalfurafine hydrochloride Nalfurafine(TRK-820) is an opioid κ-selective agonist; has been approved in Japan for treatment of itch in patients with chronic kidney disease.
T2870 (+)-Matrine Matrine, an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.
T3417 Amentoflavone Amentoflavone, as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in ...
T4351 DAMGO DAMGO is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction...
T4386 PZM21 PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
T4407 SR17018 SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
T4411 DAMGO TFA (78123-71-4(Free base)) Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines a...
T4478 CID 16020046 CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.
T4691 Asimadoline hydrochloride Asimadoline HCl is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline has also been shown to be used in the treatment of irrita...
T5158 N-Desmethylclozapine N-Desmethylclozapine is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist ...
T5167 Cebranopadol Cebranopadol 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-op...
T6175 ADL5859 HCl ADL5859 HCl is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.
T6221 Nalmefene hydrochloride Nalmefene antagonizes the effects of opioids by competing for the opioid receptors in the CNS.
T7173 [Leu5]-Enkephalin [Leu5]-Enkephalin is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and -opioid receptors (Kis = 4.0 and 3.4 nM, respectively)
T7211 Tyr-Gly-Gly-Phe-Met-OH Tyr-Gly-Gly-Phe-Met-OH, is a naturally occurring, endogenous opioid peptide that inhibits tumor growth via binding to the opioid receptor.
T7218 Endomorphin 2 Endomorphins-2 (EM-2) could decrease both the frequency and amplitude of the sEPSC of the motoneurons in lamina IX, which was reversed by the MOR antagonist CTO...
T7306 Valorphin Valorphin has opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM.
T7404 Dermorphin Dermorphin is agonist of μ-opioid receptor (MOR) agonist.
T7567 Adrenorphin(3TFA) Adrenorphin(3TFA) is an agonist of μ-opioid receptor(Ki :12 nM).
T7576 β-Casomorphin, bovine(2TFA) β-Casomorphin, bovine(2TFA) is an opioid peptide isolated from casein peptone
T7613 β-Casomorphin, human(TFA) β-Casomorphin, human(TFA) is an opioid receptor agonist.
T7637 Deltorphin I(TFA) Deltorphin I(TFA) is an agonist of δ-opioid receptor.
T7639 Deltorphin 2(TFA) Deltorphin 2(TFA) is an agonist of δ opioid receptor(IC50:0.41 nM)
T8455 Spinorphin Spinorphin is a heptapeptide, and is a potent enkephalin-degrading enzymes inhibitor.
T8557 N-terminally acetylated Leu-enkephalin Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.N-terminally acetylated Leu-enkephalin is the N-terminally ac...
T8571 ML-184 ML-184 is a potent synthetic agonist of GPR55 with EC50 of 0.26 µM.
TN3367 Akuammidine Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki v...
TN3368 Akuammigine Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding ...
TN5017 Sideritoflavone Sideritoflavone has anti-inflammatory effect, it is a selective inhibitor of lipoxygenase activity in vitro.
TP1071 Nociceptin Nociceptin is a 17-amino-acid polypeptide that is structurally related to the opioid peptide dynorphin A.
TP1254 [Met5]-Enkephalin, amide TFA [Met5]-Enkephalin, amide TFA is a δ opioid receptors agonist as well as putative ζ (zeta) opioid receptors.
TP1367 [D-Ala2]leucine-enkephalin [D-Ala2]-Leucine enkephalin is a delta opioid agonist used to study the signaling pathway of delta opioid receptors.
TP1793 Nociceptin (1-13), amide 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 mem...
TP1832 Gluten Exorphin C Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and ...
TP1905 DADLE Prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.
TQ0082 Aticaprant Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).
TQ0091 LY2795050 LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).
TQ0267 Endomorphin-1 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).
TWS0414 Cannabidiol Cannabidiol is GPR55 and weak CB1 antagonist (IC50s: 0.445 and 3.35 μM), CB2 receptor inverse agonist and inhibitor of anandamide uptake (IC50: 27.5 μM). It a...
Naloxone hydrochloride
T0102CAS 357-08-4
Naloxone hydrochloride is a specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Mirtazapine
T0137CAS 85650-52-8
Mirtazapine is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevat...
Meptazinol hydrochloride
T0201CAS 59263-76-2
Meptazinol Hcl, a unique centrally opioid analgesic, is used as a narcotic antagonist with analgesic properties.
Loperamide hydrochloride
T0209CAS 34552-83-5
Loperamide Hydrochloride is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.
Dextromethorphan HBr monohydrate
T0262CAS 6700-34-1
Methyl analog of DEXTRORPHAN that shows high-affinity binding to some areas of the brain, including the medullary cough center. This compound is an NMDA recepto...
Progesterone
T0478CAS 57-83-0
Progesterone is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY ...
Mianserin hydrochloride
T0783CAS 21535-47-7
Mianserin hydrochloride is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin ...
Trimebutine
T0918CAS 39133-31-8
Trimebutine is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid agonist eff...
Docusate sodium
T0929CAS 577-11-7
Docusate is an orally available, over-the-counter laxative and stool softener used to treat or prevent constipation. Docusate has not been linked to serum enzym...
Naltrexone hydrochloride
T0963CAS 16676-29-2
Naltrexone is a synthetic opioid antagonist used in the prevention of relapse of opiate addiction and alcoholism.
Noscapine hydrochloride
T0981CAS 912-60-7
Noscapine Hydrochloride is the orally available hydrochloride salt of the opioid agonist noscapine, a phthalide isoquinoline alkaloid derived from the opium pop...
Endomorphin 2 TFA
T11198CAS 1276124-00-5
Endomorphin 2 TFA,  displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. a high affinity, highly selective agonist of ...
GSK1521498 free base (hydrochloride)
T11478CAS 1007578-24-6
GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. GSK1521498 free base (...
GSK1521498 free base
T11478LCAS 1007573-18-3
GSK1521498 free base is a potent and selective antagonist of μ-opioid receptor. GSK1521498 free base also has the potential for disorders of compulsive consump...
GSK1521498
T11479CAS 1426543-84-1
GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and drugs. GSK1521498 is a potent and selective μ-opioid receptor (MOR)...
Naloxone benzoylhydrazone
T12168CAS 119630-94-3
Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opio...
Naltrindole hydrochloride
T12169CAS 111469-81-9
Naltrindole hydrochloride is a highly potent and selective antagonist of non-peptide δ opioid receptor(Ki of 0.02 nM).
Norbinaltorphimine dihydrochloride
T12241CAS 113158-34-2
Norbinaltorphimine dihydrochloride is a potent and selective antagonist of κ opioid receptor.
Opioid receptor modulator 1
T12314CAS 77514-44-4
Opioid receptor modulator 1 is a modulator of opioid receptor.
Alvimopan
T1242CAS 156053-89-3
Alvimopan is a synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a se...
ROCK-IN-1
T13419CAS 934387-35-6
ROCK-IN-1 is a potent ROCK inhibitor(IC50 of 1.2 nM , ROCK2).
(R,S)-Ivosidenib
T13438CAS 2070009-31-1
(R,S)-Ivosidenib is the less active enantiomer of Ivosidenib .
L-Menthol
T1407CAS 2216-51-5
L-Menthol is a levo isomer of menthol, an organic compound made synthetically or obtained from peppermint or mint oils with flavoring and local anesthetic prope...
Bevenopran
T14551CAS 676500-67-7
Bevenopran is an antagonist of peripheral μ-opioid receptor.
DPI-3290
T15165CAS 182417-73-8
DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinoci...
MCOPPB trihydrochlride
T2071CAS 1108147-88-1
MCOPPB trihydrochlride is a nociceptin receptor agonist.
Nalfurafine hydrochloride
T2388CAS 152658-17-8
Nalfurafine(TRK-820) is an opioid κ-selective agonist; has been approved in Japan for treatment of itch in patients with chronic kidney disease.
(+)-Matrine
T2870CAS 519-02-8
Matrine, an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.
Amentoflavone
T3417CAS 1617-53-4
Amentoflavone, as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in ...
DAMGO
T4351CAS 78123-71-4
DAMGO is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction...
PZM21
T4386CAS 1997387-43-5
PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
SR17018
T4407CAS 2134602-45-0
SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
DAMGO TFA (78123-71-4(Free base))
T4411CAS T4411
Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines a...
CID 16020046
T4478CAS 834903-43-4
CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.
Asimadoline hydrochloride
T4691CAS 185951-07-9
Asimadoline HCl is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline has also been shown to be used in the treatment of irrita...
N-Desmethylclozapine
T5158CAS 6104-71-8
N-Desmethylclozapine is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist ...
Cebranopadol
T5167CAS 863513-91-1
Cebranopadol 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-op...
ADL5859 HCl
T6175CAS 850173-95-4
ADL5859 HCl is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.
Nalmefene hydrochloride
T6221CAS 58895-64-0
Nalmefene antagonizes the effects of opioids by competing for the opioid receptors in the CNS.
[Leu5]-Enkephalin
T7173CAS 58822-25-6
[Leu5]-Enkephalin is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and -opioid receptors (Kis = 4.0 and 3.4 nM, respectively)
Tyr-Gly-Gly-Phe-Met-OH
T7211CAS 58569-55-4
Tyr-Gly-Gly-Phe-Met-OH, is a naturally occurring, endogenous opioid peptide that inhibits tumor growth via binding to the opioid receptor.
Endomorphin 2
T7218CAS 141801-26-5
Endomorphins-2 (EM-2) could decrease both the frequency and amplitude of the sEPSC of the motoneurons in lamina IX, which was reversed by the MOR antagonist CTO...
Valorphin
T7306CAS 144313-54-2
Valorphin has opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM.
Dermorphin
T7404CAS 77614-16-5
Dermorphin is agonist of μ-opioid receptor (MOR) agonist.
Adrenorphin(3TFA)
T7567CAS 88377-68-8
Adrenorphin(3TFA) is an agonist of μ-opioid receptor(Ki :12 nM).
β-Casomorphin, bovine(2TFA)
T7576CAS 72122-62-4
β-Casomorphin, bovine(2TFA) is an opioid peptide isolated from casein peptone
β-Casomorphin, human(TFA)
T7613CAS 102029-74-3
β-Casomorphin, human(TFA) is an opioid receptor agonist.
Deltorphin I(TFA)
T7637CAS 122752-15-2
Deltorphin I(TFA) is an agonist of δ-opioid receptor.
Deltorphin 2(TFA)
T7639CAS 122752-16-3
Deltorphin 2(TFA) is an agonist of δ opioid receptor(IC50:0.41 nM)
Spinorphin
T8455CAS 137201-62-8
Spinorphin is a heptapeptide, and is a potent enkephalin-degrading enzymes inhibitor.
N-terminally acetylated Leu-enkephalin
T8557CAS T8557
Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.N-terminally acetylated Leu-enkephalin is the N-terminally ac...
ML-184
T8571CAS 794572-10-4
ML-184 is a potent synthetic agonist of GPR55 with EC50 of 0.26 µM.
Akuammidine
TN3367CAS 639-36-1
Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki v...
Akuammigine
TN3368CAS 642-17-1
Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding ...
Sideritoflavone
TN5017CAS 70360-12-2
Sideritoflavone has anti-inflammatory effect, it is a selective inhibitor of lipoxygenase activity in vitro.
Nociceptin
TP1071CAS 170713-75-4
Nociceptin is a 17-amino-acid polypeptide that is structurally related to the opioid peptide dynorphin A.
[Met5]-Enkephalin, amide TFA
TP1254CAS TP1254
[Met5]-Enkephalin, amide TFA is a δ opioid receptors agonist as well as putative ζ (zeta) opioid receptors.
[D-Ala2]leucine-enkephalin
TP1367CAS 64963-01-5
[D-Ala2]-Leucine enkephalin is a delta opioid agonist used to study the signaling pathway of delta opioid receptors.
Nociceptin (1-13), amide
TP1793CAS 178064-02-3
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 mem...
Gluten Exorphin C
TP1832CAS 142479-62-7
Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and ...
DADLE
TP1905CAS 63631-40-3
Prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.
Aticaprant
TQ0082CAS 1174130-61-0
Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).
LY2795050
TQ0091CAS 1346133-08-1
LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).
Endomorphin-1
TQ0267CAS 189388-22-5
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).
Cannabidiol
TWS0414CAS 13956-29-1
Cannabidiol is GPR55 and weak CB1 antagonist (IC50s: 0.445 and 3.35 μM), CB2 receptor inverse agonist and inhibitor of anandamide uptake (IC50: 27.5 μM). It a...