MOR antagonist 2 hydrochloride
MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder.
For research use only. We do not sell to patients.
- CAS No.: 3075862-29-9
- Formula: C28H31ClN4O4
- Molecular Weight:523.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Opioid Receptor Isoforms
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Biological Activity
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μ Opioid Receptor/MOR 28.37 nM (IC50) |
μ Opioid Receptor/MOR 4.25 nM (EC50) |
μ Opioid Receptor/MOR 0.18 nM (Ki) |
MOR antagonist 2 hydrochloride (Compound 7) (1.5 h) exhibits high binding affinity for MOR (Ki = 0.18 nM), with 16-fold selectivity over KOR (Ki = 2.93 nM) and 169-fold selectivity over DOR (Ki = 30.44 nM) in CHO cell membrane preparations[1].
MOR antagonist 2 hydrochloride (1.5 h) acts as a low-efficacy partial agonist of MOR, with an EC50 of 4.25 nM in [35S]-GTPγS binding assays[1].
MOR antagonist 2 hydrochloride exhibits high metabolic stability in human liver S9 fractions, and shows high plasma protein binding rates in both human and mouse plasma[1].
MOR antagonist 2 hydrochloride exhibits favorable passive intestinal permeability, extremely low baseline efflux levels, and acts as a substrate for P-gp and BCRP transporters in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MOR antagonist 2 hydrochloride (0.1-5 mg/kg; s.c.; single administration) induces significantly fewer opioid withdrawal symptoms (wet dog shakes and paw tremors) in opioid-withdrawn mice than equivalent and higher doses of Naloxone (HY-17417A), while maintaining comparable μ-opioid receptor antagonist activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Webster (male, 6-8 weeks old, 25-35 g)[1]
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Dosage:10 mg/kg
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Administration:s.c.; once
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Result:Demonstrated dose-dependent antagonism of morphine-induced antinociception, with an AD50 value of 0.09 mg/kg (95% CI: 0.06-0.14 mg/kg).
Reduced the maximum possible effect (MPE) of morphine in a dose-dependent manner, with near-complete antagonism observed at 1 and 4 mg/kg.
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Animal Model:Swiss Webster (male, 6-8 weeks old, 25-35 g, morphine pellet implantation-induced opioid tolerance)[1]
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Dosage:0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg
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Administration:s.c.
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Result:Induced significantly fewer wet dog shakes than naloxone (1 mg/kg, s.c.) at 0.1 mg/kg.
Induced significantly fewer wet dog shakes and paw tremors than naloxone (1 mg/kg, s.c.) at 0.5 mg/kg, 1 mg/kg, and 5 mg/kg.
Caused significantly fewer wet dog shakes and paw tremors than naloxone at 1 mg/kg even at 5 mg/kg.
Chemical Information
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CAS No. 3075862-29-9
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Molecular Weight 523.02
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Formula C28H31ClN4O4
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SMILES
O[C@]12[C@@H]3N(CC4CC4)CC[C@@]15C6=C(C=CC(O)=C6O[C@H]5[C@H](CC2)NC(C7=NC=CC8=C7NC=C8)=O)C3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MOR antagonist 2 hydrochloride Related Classifications
HY-181605 Related Classifications
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