Search Result
Results for "
δ opioid receptor antagonists
" in MedChemExpress (MCE) Product Catalog:
-
- HY-19627A
-
|
S-297995 tosylate
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
|
-
-
- HY-76711
-
|
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight .
|
-
-
- HY-13243
-
|
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 .
|
-
-
- HY-10233
-
|
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
|
-
-
- HY-101302
-
|
|
Opioid Receptor
TRP Channel
|
Inflammation/Immunology
|
|
Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows Ki values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer .
|
-
-
- 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 .
|
-
-
- HY-145404
-
|
|
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 .
|
-
-
- HY-123689
-
|
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 .
|
-
-
- HY-76711S
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
|
-
-
- HY-P1335A
-
|
|
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 .
|
-
-
- HY-136208
-
|
|
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 .
|
-
-
- HY-19627
-
|
S-297995
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
|
-
-
- HY-101307
-
|
7-Benzylidenenaltrexone maleate
|
Opioid Receptor
|
Neurological Disease
|
|
BNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioid receptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioid receptor, respectively. BNTX maleate shows antinociceptive activity .
|
-
-
- HY-107750A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect .
|
-
-
- HY-101230
-
|
|
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 .
|
-
-
- HY-76657A
-
|
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 .
|
-
-
- HY-76711R
-
|
|
Reference Standards
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Naltrexone (Standard) is the analytical standard of Naltrexone (HY-76711). This product is intended for research and analytical applications. Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
|
-
-
- HY-16979
-
|
|
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 .
|
-
-
- HY-169867
-
|
7-Benzylidenenaltrexone
|
Opioid Receptor
|
Neurological Disease
|
|
BNTX (7-Benzylidenenaltrexone) is a highly selective δ1 opioid receptor antagonist. BNTX selectively antagonizes the antinociceptive activity mediated by spinal δ1 opioid receptors, and does not alter the antinociceptive effects mediated by δ2, μ or κ opioid receptors at selective doses .
|
-
-
- HY-107743
-
|
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 .
|
-
-
- HY-101233
-
-
-
- HY-178235
-
|
|
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 .
|
-
-
- HY-A0115R
-
|
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 .
|
-
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
-
- HY-123689S1
-
|
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 .
|
-
-
- HY-133717
-
|
|
Opioid Receptor
TRP Channel
|
Cancer
|
|
Naltriben is a selective δ2-opioid receptor antagonist and TRPM7 activator. Naltriben enhances glioblastoma cell migration and invasion. Naltriben can be used in research into neurological diseases and cancer .
|
-
-
- HY-101317A
-
|
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.
|
-
-
- HY-16765
-
|
TD-1211
|
Opioid Receptor
|
Neurological Disease
|
|
Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
|
-
-
- HY-106732
-
|
|
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 .
|
-
-
- HY-135698
-
|
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 .
|
-
-
- HY-76657
-
|
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 .
|
-
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the 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 .
|
-
-
- HY-175661
-
|
|
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 .
|
-
-
- HY-163895
-
|
|
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 .
|
-
-
- HY-123689A
-
|
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 .
|
-
-
- HY-123689S
-
|
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 .
|
-
-
- HY-123689R
-
|
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.
|
-
-
- HY-P2669
-
-
-
- HY-101199
-
|
|
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 .
|
-
-
- HY-123142
-
-
-
- HY-129422
-
-
-
- HY-177790
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin receptor antagonist 7 (Compound 34) is an antagonist of the orexin receptor (OX1R), with a Ki value of 4.05 nM. Orexin receptor antagonist 7 shows no detectable activity towards OX2R and has very low affinities for the three opioid receptors (μ, δ, κ) (Ki > 1,000 nM). Orexin receptor antagonist 7 can be used for research on opioid addiction .
|
-
-
- HY-16765A
-
|
TD-1211 sulfate
|
Opioid Receptor
|
Neurological Disease
|
|
Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
|
-
-
- HY-107750
-
-
-
- HY-118615
-
|
|
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 .
|
-
-
- HY-107745
-
-
-
- HY-13243R
-
|
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 .
|
-
-
- HY-117881
-
|
|
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 .
|
-
-
- HY-76657AR
-
|
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 .
|
-
-
- HY-P5892
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-11052A
-
|
|
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 .
|
-
- HY-P2429
-
|
|
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.
|
-
- HY-172149
-
|
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) .
|
-
- HY-170437
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Kis of 0.25, 41.1, 1.30 nM, respectively[1]
|
-
- HY-118949
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-119733
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
|
-
- HY-101343
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
|
-
- HY-10233R
-
|
Lu 02-030 hydrochloride (Standard); THIP hydrochloride (Standard)
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
|
-
- HY-179282
-
|
|
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) .
|
-
- HY-13243S1
-
|
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 .
|
-
- HY-125790
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Cyclazocine is a μ, δ, and κ opioid receptor modulator with Ki values of 0.32, 1.1, and 0.18 nM, respectively. Cyclazocine exhibits "mixed" pharmacological activities, acting as a μ-partial antagonist, κ-agonist, and low-affinity δ ligand. Cyclazocine shows antinociceptive activity in mice. Cyclazocine can be used in studies on psychoactive substance addiction .
|
-
-
- 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 .
|
-
- HY-P1335A
-
|
|
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 .
|
-
- HY-101230
-
|
|
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 .
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the 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 .
|
-
- HY-P2669
-
-
- HY-129422
-
-
- HY-P5892
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-P2429
-
|
|
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.
|
| 製品番号 |
製品名 |
Category |
Target |
構造式 |
-
- HY-76711S
-
|
|
Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
|
-
-
- HY-123689S1
-
|
|
|
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 .
|
-
-
- HY-123689S
-
|
|
|
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 .
|
-
-
- HY-13243S1
-
|
|
|
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 .
|
-
入力情報は安全に管理されます. ※ 必須入力項目.
Inquiry Information
- 製品名:
- 製品番号:
- 数量:
- MCE 日本正規代理店: