AT2 receptor agonist C21

An AT2 receptor agonist

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5mg

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Background

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 (K_is = 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)