Synthesis, receptor binding, and activation studies of N (1)-alkyl-l-histidine containing thyrotropin-releasing hormone (TRH) analogues

…, V Monga, JS Josan, X Lu, MC Gershengorn…

Index: Kaur, Navneet; Monga, Vikramdeep; Josan, Jatinder S.; Lu, Xinping; Gershengorn, Marvin C.; Jain, Rahul Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 17 p. 5981 - 5988

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Citation Number: 17

Abstract

Thyrotropin-releasing hormone (TRH) analogues in which the N (1)-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). Analogue 3 (R= C2H5) exhibited binding affinity (Ki) of 0.012 μM to TRH-R1 that is about 1.1-fold higher than that of TRH. Several analogues were found to selectively ...