CGP42112: the full AT2 receptor agonist and its role in the renin-angiotensin-aldosterone system: no longer misunderstood.
CGP42112: the full AT2 receptor agonist and its role in the renin-angiotensin-aldosterone system: no longer misunderstood.
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DOI：
10.1042/cs20220261
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发表时间：
2022-11-11
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多年来，AT2R 选择性配体 CGP42112 一直被错误地描述为部分激动剂，部分原因是它在高浓度下也能与 AT1R 相互作用。直到2009年，它仍然被视为对手。在这篇观点/意见文章中，我们试图通过广泛回顾文献来解决围绕该化合物功效的模糊性，追溯到 1989 年，表明 CGP42112 从未被令人信服地证明是 AT2R 的部分激动剂或拮抗剂。虽然 CGP42112 现在通常被定性为 AT2R 激动剂，但遗憾的是，很少有研究可以验证其作为 AT2R 完全激动剂的功效，这为继续猜测其功效程度留下了空间。希望这篇观点/意见文章中提供的信息将牢固地确立 CGP42112 作为 AT2R 的完全激动剂，以便它可以再次用作研究 AT2R 的工具。
For years, the AT2R-selective ligand CGP42112 has been erroneously characterized as a partial agonist, partly due to its ability to also interact with the AT1R at high concentrations. As late as 2009, it was still being characterized as an antagonist as well. In this perspective/opinion piece, we try to resolve the ambiguity that surrounds the efficacy of this compound by extensively reviewing the literature, tracing its beginnings to 1989, showing that CGP42112 has never been convincingly shown to be a partial agonist or an antagonist at the AT2R. While CGP42112 is now routinely characterized as an AT2R agonist, regrettably, there is a paucity of studies that can validate its efficacy as a full agonist at the AT2R, leaving the door open for continuing speculation regarding the extent of its efficacy. Hopefully, the information presented in this perspective/opinion piece will firmly establish CGP42112 as a full agonist at the AT2R such that it can once again be used as a tool to study the AT2R.