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TargetMol | Tags Endocrinology/Hormones
TargetMol | Tags GPCR/G Protein
TargetMol | Tags Neuroscience

Opioid Receptor

Opioid receptors belong to the large superfamily of seven transmembrane-spanning (7TM) G protein-coupled receptors (GPCRs). As a class, GPCRs are of fundamental physiological importance mediating the actions of the majority of known neurotransmitters and hormones.

  • BTRX-335140
    T148352244614-14-8
    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 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) . BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.
    • $107
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  • DAMGO TFA (78123-71-4(Free base))
    T4411
    Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines and chemokine receptors through TGF-beta1. Increases food intake of rats.
    • $57
    Backorder
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    TargetMol | Inhibitor Hot
  • Aticaprant
    TQ00821174130-61-0
    Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).
    • $34
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    TargetMol | Inhibitor Hot
  • Mianserin hydrochloride
    T078321535-47-7
    Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. It may cause drowsiness and hematological problems.
    • $32
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  • CP 866087
    T31081L519052-02-9In house
    CP 866087 is an opioid receptor antagonist for the study of female sexual dysfunction.
    • $195 TargetMol
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  • CP-866087
    T31081519052-04-1In house
    CP-866087 is a novel, potent and selective mu-opioid receptor antagonist for the study of female sexual dysfunction.
    • $762
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  • Docusate sodium
    T0929577-11-7
    Docusate sodium (Aerosol OT) is an orally available, over-the-counter laxative and stool softener used to treat or prevent constipation. Docusate has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury with jaundice.
    • $36
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  • Amentoflavone
    T34171617-53-4
    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.
    • $30
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    TargetMol | Citations Cited
  • JTC-801
    T6553244218-51-7
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
    • $41
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  • Faxeladol
    T31750433265-65-7In house
    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.
    • $628
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  • Dynorphin A acetate(80448-90-4 free base)
    TP2040L
    Dynorphin A acetate is an Endogenous kappa receptor agonist.
    • $65
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  • Dermorphin TFA
    T774878331-26-7
    Dermorphin TFA is a new class of opioids-like peptides
    • $92
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  • [Leu5]-Enkephalin, amide acetate
    TP1113L
    [Leu5]-Enkephalin, amide acetate is a δ opioid receptor agonist.
    • $32
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  • Adrenorphin 3TFA(88377-68-8(free base))
    T7567L
    Adrenorphin 3TFA(88377-68-8(free base)) (Metorphamide) is an agonist of μ-opioid receptor(Ki :12 nM).
    • $68
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  • Dynorphin A 1-10 acetate(79994-24-4 free base)
    TP1813L
    Dynorphin A (1-10) acetate is an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    • $101
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  • Ac-RYYRIK-NH2 acetate
    TP1940L1
    Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.
    • $295
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  • Dynorphin B (1-13) acetate(83335-41-5 free base)
    TP1826L
    Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.
    • $156
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  • β-Endorphin (1-27) (human) acetate
    T38193L
    β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid
    • $195
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  • [DPro10] Dynorphin A (1-11)acetate,porcine
    T76341L
    [DPro10] Dynorphin A (1-11)acetate,porcine is a highly potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine is an n-alkylated derivative with analgesic activity.
    • $55
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  • beta-Neoendorphin acetate(77739-21-0 free base)
    TP2322L78658-39-6
    beta-Neoendorphin acetate is an agonist of κ-opioid receptor
    • $133
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  • SCH-486757
    T28728524019-25-8In house
    SCH-486757 is an agonist of nociceptin-1 (NOP1) and orphanin FQ peptide receptors and is used in the study of cough.
    • $293 TargetMol
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  • Nociceptin (1-7) acetate
    T23076L
    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.
    • $326
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  • Propiram fumarate HCl
    T28453L945013-73-0In house
    Propiram fumarate HClis an orally available Opioid receptors agonist with analgesic activity for the study of musculoskeletal pain.
    • $195
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  • Leuphasyl TFA
    T20435L67586-27-0
    Leuphasyl TFA is an amid peptide, a δ-opioid receptor agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors. Leuphasyl TFA is a potent, long-acting Leu-enkephalin analog that is resistant to enzymatic degradation
    • $133
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  • DuP 747 HCl
    T25354L115904-74-0In house
    DuP 747 HCl is a selective kappa agonist with analgesic activity.DuP 747 consists of two conformations.
    • $258
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  • Difelikefalin acetate
    TP2501
    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.
    • $167
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  • UFP-101 acetate
    TP2105L
    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.
    • $317
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  • ADL-5747
    T29663850176-30-6In house
    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.
    • $143
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  • difelikefalin acetate(1024828-77-0 Free base)
    TP2485
    is a ketone and a building block.
    • $167
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  • (D-Ser2)-Leu-Enkephalin-Thr
    T22752L
    (D-Ser2)-Leu-Enkephalin-Thr is a delta selective agent of opioid receptor and shows analgesic effects.
    • $68
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  • β-Casomorphin, bovine TFA(72122-62-4(free base))
    T7576L
    β-Casomorphin, bovine TFA is an opioid peptide isolated from casein peptone
    • $37
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  • Samidorphan HCl
    T67888L2328045-02-7In house
    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.
    • $167
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  • CTAP(TFA) (103429-32-9 free base)
    TP2050L
    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)
    • $205
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  • SCH 221510
    T23335322473-89-2In house
    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.
    • $143
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  • [(pF)Phe4]Nociceptin(1-13)NH2 acetate
    TP1885L1
    [(pF)Phe4]Nociceptin(1-13)NH2 acetate is a selective agonist of NOP receptor with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 acetate displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).
    • $327
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  • [Leu5]-Enkephalin acetate(58822-25-6 free base)
    T7173L
    [Leu5]-Enkephalin acetate(58822-25-6 free base) 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)
    • $51
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  • Trimebutine CTB salt
    T274131456509-46-8In house
    Trimebutine CTB salt (GIC-1001) is an opioid receptor agonist used in the study of pain.
    • $293 TargetMol
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  • Porcine dynorphin A(1-13) acetate
    TP1179L
    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.
    • $68
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  • Deltorphin
    T20166119975-64-3
    Deltorphin (Dermenkephalin) is Isolated from the skin of Phyllomedusa Sauvage. It also has an affinity to the opioid receptor.
    • $173
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  • Endomorphin 2
    T7218141801-26-5
    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 CTOP. EM-2-IR fibers originated from primary afferent fibers form symmetric synaptic connections with motoneurons innervating skeletal muscles of the lower limbs in lamina IX of the spinal ventral horn and EM-2 might exert inhibitory effects on the activities of these motoneurons through both presynaptic and postsynaptic mechanisms.
    • $41
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  • JNJ-20788560
    T27667825649-28-3In house
    JNJ-20788560 is a delta opioid receptor (DOR) agonist with analgesic activity. It is more selective for DOR than for mu opioid receptors (MOR).
    • $350
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  • Hemorphin-7 acetate(152685-85-3 free base)
    TP1404L
    Hemorphin-7 acetate is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
    • $108
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  • Deltorphin 2
    T7639122752-16-3
    Deltorphin 2 ([D-Ala2]-Deltorphin II) is an agonist of δ opioid receptor with an IC50 of 1 nM.
    • $57
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    TargetMol | Citations Cited
  • Neuropeptide AF (human) acetate
    TP1082L
    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.
    • $180
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  • Nociceptin (1-13) amide TFA
    TP1793L
    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.
    • $133
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  • b-Casomorphin (1-3) Acetate
    T21660L
    b-Casomorphin (1-3) Acetate is a tri-peptide with an opioid effect.
    • $30
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  • Orphanin FQ(1-11) acetate(178249-41-7 free base)
    TP1882L1
    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.
    • $162
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  • CTOP acetate
    TP2052L
    CTOP acetate is a somatostatin analogue and a μ-opioid receptor antagonist.
    • $227
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  • ORL1 antagonist 1
    T123201174985-59-1In house
    ORL1 antagonist 1 is an o antagonist of pioid receptor-like 1 (ORL1) (IC50 of 61 nM).
    • $117
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  • BAM 22P acetate
    TP1211L
    BAM 22P acetate is a potent opioid agonist.
    • $257
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