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Results for "

δ-opioid receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

36

Inhibitors & Agonists

6

Peptides

1

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13243
    Alvimopan
    2 Publications Verification

    ADL 8-2698; LY 246736

    		 Opioid Receptor Neurological Disease
    Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
    Alvimopan
  • HY-145404
    Mitragynine pseudoindoxyl
    1 Publications Verification

    		 Opioid Receptor Metabolic Disease
    Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .
    Mitragynine pseudoindoxyl
  • HY-P1335
    CTAP
    2 Publications Verification

    		 Opioid Receptor Neurological Disease
    CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP 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) and opiate overdose or addiction .
    CTAP
  • HY-123689
    Samidorphan

    ALKS-33; RDC-0313

    		 Opioid Receptor Neurological Disease
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals .
    Samidorphan
  • HY-136208
    TAN-452

    		Opioid Receptor Neurological Disease
    TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
    TAN-452
  • HY-P1335A
    CTAP TFA
    2 Publications Verification

    		 Opioid Receptor Neurological Disease
    CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
    CTAP TFA
  • HY-101230
    ICI 174864

    		Opioid Receptor Neurological Disease
    ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with Ke values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways .
    ICI 174864
  • HY-76657A
    Alvimopan dihydrate
    2 Publications Verification

    ADL 8-2698 dihydrate; LY 246736 dihydrate

    		 Opioid Receptor Neurological Disease Cancer
    Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
    Alvimopan dihydrate
  • HY-16979
    TRK-851

    		Opioid Receptor Neurological Disease
    RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects .
    TRK-851
  • HY-101233
    ICI 154129

    M 154129

    		 Opioid Receptor Neurological Disease
    ICI 154 129 is a delta-opioid receptor antagonist and can be used for seizure research.
    ICI 154129
  • HY-178235
    MDAN-21

    		Opioid Receptor Neurological Disease
    MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia .
    MDAN-21
  • HY-A0115R
    Ramiprilat (Standard)

    HOE 498 diacid (Standard); Ramipril diacid (Standard)

    		 Drug Metabolite Reference Standards Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
    Ramiprilat (Standard)
  • HY-107743
    Naloxone benzoylhydrazone

    NalBzoH

    		 Opioid Receptor Neurological Disease
    Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. 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 opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect .
    Naloxone benzoylhydrazone
  • HY-163895
    δ opioid receptor antagonist 1

    		Fluorescent Dye Opioid Receptor Neurological Disease
    δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception .
    δ opioid receptor antagonist 1
  • HY-123689S1
    Samidorphan-d5

    ALKS-33-d5; RDC-0313-d5

    		 Isotope-Labeled Compounds Opioid Receptor Neurological Disease
    Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
    Samidorphan-d5
  • HY-76657
    Alvimopan monohydrate

    ADL 8-2698 monohydrate; LY 246736 monohydrate

    		 Opioid Receptor Neurological Disease Cancer
    Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus .
    Alvimopan monohydrate
  • HY-107745
    SDM25N hydrochloride

    		Opioid Receptor Flavivirus Infection Neurological Disease
    SDM25N hydrochloride, a δ-opioid receptor antagonist, is a potent DENV inhibitor. SDM25N hydrochloride targets the viral NS4B protein and restricts genomic RNA replication .
    SDM25N hydrochloride
  • HY-106732
    AT-076

    		Opioid Receptor Neurological Disease
    AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioid receptors, with Ki values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively .
    AT-076
  • HY-135698
    Methocinnamox

    M-CAM

    		 Opioid Receptor Neurological Disease
    Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .
    Methocinnamox
  • HY-101317A
    TAN-67

    SB-205607

    		 Opioid Receptor Metabolic Disease
    TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
    TAN-67
  • HY-175661
    SRI-22136

    		Opioid Receptor Beta-secretase Neurological Disease
    SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease .
    SRI-22136
  • HY-123689A
    Samidorphan hydrochloride

    ALKS-33 hydrochloride; RDC-0313 hydrochloride

    		 Opioid Receptor Neurological Disease
    Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals .
    Samidorphan hydrochloride
  • HY-123689S
    Samidorphan-d4

    ALKS-33-d4; RDC-0313-d4

    		 Isotope-Labeled Compounds Opioid Receptor Neurological Disease
    Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
    Samidorphan-d4
  • HY-123689R
    Samidorphan (Standard)

    ALKS-33 (Standard); RDC-0313 (Standard)

    		 Opioid Receptor Reference Standards Neurological Disease
    Samidorphan (Standard) is the analytical standard of Samidorphan. This product is intended for research and analytical applications. Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals.
    Samidorphan (Standard)
  • HY-101199
    N-Benzylnaltrindole hydrochloride

    		Opioid Receptor Neurological Disease
    N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function .
    N-Benzylnaltrindole hydrochloride
  • HY-P2429
    N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu

    		Opioid Receptor Others
    N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a compound that can antagonize the δ-opioid receptor and the action of [D-Pen2,D-Pen ] enkephalin in vivo. Its antagonistic effect can be verified by specific behavioral experiments.
    N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu
  • HY-P2669
    Boc-YPGFL(O-tBu)

    		Opioid Receptor Neurological Disease
    Boc-YPGFL(O-tBu) is a selective δ opioid receptor (DOR) peptide antagonist .
    Boc-YPGFL(O-tBu)
  • HY-11052A
    Trap-101 hydrochloride

    		Opioid Receptor Neurological Disease
    Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
    Trap-101 hydrochloride
  • HY-13243R
    Alvimopan (Standard)

    ADL 8-2698 (Standard); LY 246736 (Standard)

    		 Opioid Receptor Reference Standards Neurological Disease Cancer
    Alvimopan (Standard) is the analytical standard of Alvimopan. This product is intended for research and analytical applications. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
    Alvimopan (Standard)
  • HY-129422
    Diallyl G

    		Opioid Receptor Neurological Disease
    Diallyl G is a delta-opioid receptor antagonist. Diallyl G shows inhibitory effect on GTPase .
    Diallyl G
  • HY-76657AR
    Alvimopan dihydrate (Standard)

    ADL 8-2698 dihydrate (Standard); LY 246736 dihydrate (Standard)

    		 Reference Standards Opioid Receptor Neurological Disease Cancer
    Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
    Alvimopan dihydrate (Standard)
  • HY-117881
    CJ-15208

    		Opioid Receptor Neurological Disease
    CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
    CJ-15208
  • HY-118615
    LY2048978

    		Opioid Receptor Neurological Disease
    LY2048978 is a non-selective opioid receptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder .
    LY2048978
  • HY-172149
    Naltrindole 5′-isothiocyanate

    5'-NTII

    		 Opioid Receptor Neurological Disease
    Naltrindole 5′-isothiocyanate (5'-NTII) is a non-selective delta opioid receptor antagonist that can antagonize the analgesic effects induced by DSLET (HY-P1332) without affecting the analgesic effects induced by DPDPE (HY-P1334) .
    Naltrindole 5′-isothiocyanate
  • HY-13243S1
    Alvimopan-d7

    ADL 8-2698-d7; LY 246736-d7

    		 Isotope-Labeled Compounds Opioid Receptor Neurological Disease Cancer
    Alvimopan-d7 (ADL 8-2698-d7) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
    Alvimopan-d7
  • HY-179282
    Mu opioid receptor antagonist 9

    		Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD) .
    Mu opioid receptor antagonist 9

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