AGN-201781
AGN-201781 is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain.
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- CAS No.: 628730-30-3
- Formule: C9H12N2S
- Masse moléculaire:180.27
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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
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
AGN-201781 (compound 11) acts as a potent α-2B-preferring adrenergic agonist with no detectable activity at α-2A receptors, weak activity at α-2C receptors, minimal activity at α-1A receptors, and no activity at α-1B or α-1D receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AGN-201781 (1 mg/kg; i.p.; single dose; 0.5 mg/kg; i.v.; single dose; 3 mg/kg; p.o.; single dose) does not produce significant sedative or cardiovascular side effects at doses higher than those required for peak neuropathic pain relief in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 100-120 grams for acute dosing; neuropathic pain Chung model via partial ligation of left spinal nerves L-5 and L-6)[1]
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Dosage:30-1000 μg/kg (acute oral); 0.1 mg/kg/hour (extended subcutaneous)
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Administration:p.o.; single dose (acute); subcutaneous osmotic minipump; continuous; 5 days (extended)
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Result:Produced no significant allodynia reversal at 30 μg/kg.
Produced 60-90% peak allodynia reversal at 100 μg/kg and 300 μg/kg, with effects diminishing by 140 minutes post-dose.
Produced lower peak allodynia reversal at 1000 μg/kg, with effects diminishing over time.
Achieved ~80% allodynia reversal during 5-day continuous dosing, with analgesic effect maintained at the same level for 30 days post-dosing.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 628730-30-3
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Masse moléculaire 180.27
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Formule C9H12N2S
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SMILES
S=C1NC=C(N1)CC2CC=CC2
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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)
AGN-201781 Related Classifications
HY-100323 Related Classifications
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