Document Report Card

ID: ALA1141095

Journal: J Med Chem

Title: Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.

Authors: Kaur N, Lu X, Gershengorn MC, Jain R.

Abstract: 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.

CiteXplore: 16162016

DOI: 10.1021/jm0505462