KOR agonist 8
KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research.
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- Formule: C38H44N2O3
- Masse moléculaire:576.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
KOR agonist 8 (Compound 8a) (30 min) displays high, selective binding affinity for KOR in CHO cell membranes, with a Ki of 5.3 nM and over 100-fold selectivity over MOR and DOR[1].
KOR agonist 8 (Compound 8a) (15 min) potently inhibits cAMP production via KOR activation in HEK293-hKOR-GloSensor cells, with an EC50 of 43.1 nM, indicating strong G protein signaling efficacy[1].
KOR agonist 8 (Compound 8a) (17 h) exhibits very low potency for β-arrestin recruitment via KOR in HTLA cells, with an EC50 of 9236 nM, leading to >200-fold functional selectivity for G protein signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KOR agonist 8 (0.2-2 mg/kg; i.p.; single dose) exhibits dose-dependent antinociceptive activity in the mouse abdominal constriction test, with an ED50 of 0.5 mg/kg (i.p.) at 3 hours post-administration[1].
KOR agonist 8 (2-105 mg/kg; i.p.; single dose) induces dose-dependent motor impairment in the mouse rotarod test, with effects ranging from slight impairment at 2 mg/kg to pronounced impairment at doses up to 105 mg/kg (i.p.)[1].
Compound 8a (20 mg/kg; i.p.; single dose) significantly reduces novelty-induced locomotor activity in mice during two post-administration intervals[1].
Compound 8a (20 mg/kg; i.p.; single dose) induces significant conditioned place aversion in mice at both 1 hour and 3 hours post-administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (female, 18-20 g)[1]
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Dosage:0.2, 2, 10, 20 mg/kg
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Administration:i.p.; single dose
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Result:Produced dose-dependent antinociceptive effects, with an ED50 of 8.2 mg/kg (95% confidence limits: 6.3-10.6 mg/kg) at 3 hours post-administration.
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Animal Model:ICR mice (male, 18-20 g)[1]
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Dosage:0.2, 0.5, 1, 2 mg/kg
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Administration:i.p.; single dose
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Result:Produced dose-dependent antinociceptive effects, with an ED50 of 0.5 mg/kg (95% confidence limits: 0.3-0.8 mg/kg).
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Animal Model:ICR mice (male, 18-20 g)[1]
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Dosage:2, 10, 20, 105 mg/kg
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Administration:i.p.; single dose
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Result:Produced a slight reduction in latency to fall at 2 mg/kg, with progressively more pronounced dose-dependent impairment at higher doses up to 105 mg/kg.
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Animal Model:ICR mice (male, 18-20 g)[1]
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Dosage:20 mg/kg
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Administration:i.p.; single dose
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Result:Significantly reduced locomotor activity during both the 0.5-1.5 hour and 2.5-3.5 hour intervals post-administration.
Chemical Information
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Masse moléculaire 576.77
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Formule C38H44N2O3
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SMILES
CN(CC1=CC=CC=C1)C2=CC([C@@H](C3)[C@@]4(OC)[C@H]5[C@@]6([C@@]3(CC4)C(N(CC6)CC7CC7)C8)C9=C8C=CC(OC)=C9O5)=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KOR agonist 8 Related Classifications
HY-181515 Related Classifications
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