An AT2 receptor agonist
AT2 agonist C21 is an agonist of the angiotensin II type 2 (AT2) receptor.1 It selectively binds to the AT2 receptor over the AT1 receptor (Kis = 0.4 and >10 ?M, respectively). AT2 agonist C21 (0.1 ?M) induces neurite outgrowth in NG 108-15 cells. It reduces mean arterial blood pressure in anaesthetized spontaneously hypertensive rats (SHRs) when administered at a dose of 0.05 mg/kg. AT2 agonist C21 (0.03 mg/kg) reduces right ventricle hypertrophy and fibrosis, as well as lung interstitial and perivascular fibrosis, in a rat model of pulmonary hypertension induced by monocrotaline .2 It increases survival and reduces neurological deficits in a mouse model of cerebral ischemia induced by middle cerebral artery occlusion (MCAO) when administered at the same dose.3
1.Wan, Y., Wallinder, C., Plouffe, B., et al.Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonistJ. Med. Chem.47(24)5995-6008(2004) 2.Bruce, E., Shenoy, V., Rathinasabapathy, A., et al.Selective activation of angiotensin AT2 receptors attenuates progression of pulmonary hypertension and inhibits cardiopulmonary fibrosisBr. J. Pharmacol.172(9)2219-2231(2004) 3.Schwengel, K., Namsolleck, P., Lucht, K., et al.Angiotensin AT2-receptor stimulation improves survival and neurological outcome after experimental stroke in miceJ. Mol. Med. (Berl.)94(8)957-966(2016)
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