对促甲状腺激素释放激素受体亚型2具有选择性的促甲状腺激素释放激素（TRH）类似物。
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
作者信息
Kaur Navneet, Lu Xinping, Gershengorn Marvin C, Jain Rahul
机构信息
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar--160 062, Punjab, India.
出版信息
J Med Chem. 2005 Sep 22;48(19):6162-5. doi: 10.1021/jm0505462.
Thyrotropin-releasing hormone (TRH) analogues in which the C-2 position of the imidazole ring of the centrally placed histidine residue is substituted with various alkyl groups were synthesized and studied as agonists for TRH receptor subtype 1 (TRH-R1) and subtype 2 (TRH-R2). Several analogues were found to be selective agonists for TRH-R2 exhibiting no activation of TRH-R1. For example, analogue 4 (R= c-C3H5) was found to activate TRH-R2 with a potency (EC50) of 0.41 microM but did not activate TRH-R1 (potency > 100 microM). This study describes the first discovery of TRH-R2-specific agonists and provides impetus to design predominately CNS-effective TRH peptides.
合成了组氨酸残基位于中心的咪唑环C-2位被各种烷基取代的促甲状腺激素释放激素（TRH）类似物，并将其作为TRH受体1型（TRH-R1）和2型（TRH-R2）的激动剂进行研究。发现几种类似物是TRH-R2的选择性激动剂，对TRH-R1无激活作用。例如，发现类似物4（R = c-C3H5）以0.41 microM的效力（EC50）激活TRH-R2，但不激活TRH-R1（效力> 100 microM）。本研究首次发现了TRH-R2特异性激动剂，并为设计主要对中枢神经系统有效的TRH肽提供了动力。
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