Thyrotropin-releasing hormone receptors


Thyrotropin-releasing hormone (TRH) receptors are activated by the endogenous tripeptide TRH (pGlu-His-ProNH2). TRH and TRH analogues fail to distinguish TRH1 and TRH2 receptors [1]. [3H]TRH (human, mouse, rat) is able to label both TRH1 and TRH2 receptors with Kd values of 13 and 9 nM respectively. Synthesis and biology of ring-modified L-Histidine containing TRH analogues has been reported [2].


  1. Sun Y, Lu X, Gershengorn MC. Thyrotropin-releasing hormone receptors -- similarities and differences. J Mol Endocrinol 2003;30:87-97.
  2. Meena CL, Thakur A, Nandekar PP, et al. Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues. Eur J Med Chem 2016;111:72-83.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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