AT₂ Agonist C21

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 µM, respectively). AT₂ agonist C21 (0.1 µM) 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 (MCT; Item No. 16666).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

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1. Wan, Y., Wallinder, C., Plouffe, B., et al. Design, synthesis, and biological evaluation of the first selective nonpeptide AT₂ receptor agonist. J. 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 fibrosis. Br. 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 mice. J. Mol. Med. (Berl.) 94(8), 957-966 (2016).