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^[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]. 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].