RO27-3225 TFA 是一种有效的选择性黑皮质素 4 受体 (MC4R) 激动剂，对于 MC4R 和 MC1R 的 EC50 分别为 1 nM 和 8 nM。RO27-3225 TFA 对 MC4R 的选择性是 MC3R 的 30 倍左右。RO27-3225 TFA 具有神经保护和抗炎作用。
RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects[1][2][3].
[1]. Benoit SC, et al. A novel selective melanocortin-4 receptor agonist reduces food intake in rats and mice without producing aversive consequences. J Neurosci. 2000 May 1;20(9):3442-8. [2]. Giuliani D, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol. 2007 Mar;150(5):595-603. [3]. Zhang Y, et al. Effects of RO27-3225 on neurogenesis, PDGFRβ+ cells and neuroinflammation after cerebral infarction. Int Immunopharmacol. 2020 Feb 11;81:106281.
动态评分
0.0