2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. AGN-201781

AGN-201781 (compound 11) is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain.

For research use only. We do not sell to patients.

AGN-201781

AGN-201781 Chemical Structure

CAS No. : 628730-30-3

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AGN-201781 Related Antibodies

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Description

AGN-201781 (compound 11) is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain[1].

In Vitro

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 Related Antibodies
In Vivo

AGN-201781 (compound 11) (30-1000 μg/kg; p.o.; single dose; 0.1 mg/kg/hour; subcutaneous osmotic minipump; continuous; 5 days) produces significant acute neuropathic pain relief at oral doses of 100 μg/kg and higher, and maintains ~80% allodynia reversal for at least 30 days following 5 days of continuous subcutaneous administration[1].
AGN-201781 (compound 11) (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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 30-1000 μg/kg (acute oral); 0.1 mg/kg/hour (extended subcutaneous)
Administration: p.o.; single dose (acute); subcutaneous osmotic minipump; continuous; 5 days (extended)
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.
Clinical Trial
Molecular Weight

180.27

Formula

C9H12N2S
CAS No.
SMILES

S=C1NC=C(N1)CC2CC=CC2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AGN-201781 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AGN-201781628730-30-3AGN201781AGN 201781Adrenergic ReceptorBeta Receptorneuropathic painpost-operative painα-2B adrenergic receptorinflammatory painperipheral analgesiacancer-related painvisceral painbrimonidineα-2C adrenergic receptorsα-2A adrenergic receptorsInhibitorinhibitorinhibit

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