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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.

DAMGO TFA (78123-71-4(Free base))
T4411
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.
  • $57
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ZT 52656A hydrochloride
T13414115730-24-0
ZT 52656A is a selective agonist of kappa opioid, and used for the prevention or alleviation of pain in the eye.
  • $569
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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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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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Apitegromab
T774452278276-46-1
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.
  • $222
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DAMGO
T435178123-71-4
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.
  • $43
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SNC 80
T8414156727-74-1In house
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.
  • $35
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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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LY2940094
T157991307245-86-8
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).
  • $74
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Salvinorin A
T2330683729-01-5
Salvinorin A is a non-nitrogenous κ-opioid selective agonist.
    Inquiry
    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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    Dynorphin A acetate(80448-90-4 free base)
    TP2040L
    Dynorphin A acetate is an Endogenous kappa receptor agonist.
    • $65
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    BMS986187
    T8991684238-37-7
    BMS986187 is a novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Receptor.
    • $33
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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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    Aticaprant
    TQ00821174130-61-0
    Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]
    • $34
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    Mirtazapine
    T013785650-52-8
    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.
    • $34
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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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    PZM21
    T43861997387-43-5
    PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
    • $39
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    BMS-986122
    T26869313669-88-4
    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).
    • $41
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    NNC 63-0532
    T23074250685-44-0
    NNC 63-0532 is a potentnociceptin receptor agonist, Ki=7.3 nM, EC50=305 nM.
    • $42
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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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    Loperamide hydrochloride
    T020934552-83-5
    Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.
    • $50
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    BTRX-335140
    T148352244614-14-8
    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.
    • $107
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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.
    • $80
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    Alvimopan
    T1242156053-89-3
    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.
    • $45
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    Asimadoline hydrochloride
    T4691185951-07-9
    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.
    • $30
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    difelikefalin acetate(1024828-77-0 Free base)
    TP2485
    is a ketone and a building block.
    • $167
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    ADL-5859
    T6175850173-95-4
    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.
    • $38
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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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    Meptazinol hydrochloride
    T020159263-76-2
    Meptazinol hydrochloride (Meptazinol HCl) , a unique centrally opioid analgesic, is used as a narcotic antagonist with analgesic properties.
    • $41
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    Naltrexone hydrochloride
    T096316676-29-2
    Naltrexone hydrochloride (Naltrexone HCl) is a synthetic opioid antagonist used in the prevention of relapse of opiate addiction and alcoholism.
    • $50
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    Endomorphin 1
    TQ0267189388-22-5
    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).
    • $45
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    Deltorphin I
    T7637122752-15-2
    Deltorphin I is an agonist of δ-opioid receptor.
    • $58
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    IPAG
    T22870193527-91-2
    IPAG is a potent σ-receptor antagonist (pKi=4.3). IPAG can induce cell apoptosis.
    • $32
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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.
    • $100
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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.
    • $39
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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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    Norbinaltorphimine dihydrochloride
    T12241113158-34-2In house
    Norbinaltorphimine dihydrochloride is a selective and potent κ opioid receptor antagonist that induces itch-associated responses in mice.
    • $34
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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.
    • $41
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    Dermorphin
    T740477614-16-5
    Dermorphin is agonist of μ-opioid receptor (MOR) agonist.
    • $37
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    Nociceptin
    TP1071170713-75-4
    Nociceptin (Orphanin FQ) is a 17-amino-acid polypeptide that is structurally related to the opioid peptide dynorphin A.
    • $74
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    BW-180C
    TP190563631-40-3
    BW-180C (DADLE) is a prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.
    • $39
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    BRL 52537 hydrochloride
    T21757112282-24-3
    BRL 52537 hydrochloride is a selective and specific KOR agonist which has been implicated in neuroprotection from ischemic neuronal injury[1]. It is used for research into potential treatments for stroke and heart attack as well as more general brain rese
    • $34
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    Corydaline
    T5S2360518-69-4
    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.
    • $55
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    Endomorphin 1 acetate
    T724231276123-71-7
    Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects. Endomorphin 1 acetate shows high affinity for kappa3 and can be used to study neurological diseases.
    • $37
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    Methylnaltrexone bromide
    T2142273232-52-7
    Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.
    • $47
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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.
    • $34
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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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