β-Arrestin-Biased AT(1) Agonist TRV027 Causes a Neonatal-Specific Sustained Positive Inotropic Effect Without Increasing Heart Rate

β-arrestin 偏向性 AT(1) 激动剂 TRV027 可引起新生儿特异性的持续性正性肌力作用,且不增加心率

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Abstract

The treatment of pediatric heart failure is a long-standing unmet medical need. Angiotensin II supports mammalian perinatal circulation by activating cardiac L-type Ca(2+) channels through angiotensin type 1 receptor (AT(1)R) and β-arrestin. TRV027, a β-arrestin-biased AT(1)R agonist, that has been reported to be safe but not effective for adult patients with heart failure, activates the AT(1)R/β-arrestin pathway. We found that TRV027 evokes a long-acting positive inotropic effect specifically on immature cardiac myocytes through the AT(1)R/β-arrestin/L-type Ca(2+) channel pathway with minimum effect on heart rate, oxygen consumption, reactive oxygen species production, and aldosterone secretion. Thus, TRV027 could be utilized as a valuable drug specific for pediatric heart failure.

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