Title |
Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor
|
---|---|
Published in |
Frontiers in endocrinology, January 2012
|
DOI | 10.3389/fendo.2012.00120 |
Pubmed ID | |
Authors |
Nanthakumar Thirunarayanan, Bruce M. Raaka, Marvin C. Gershengorn |
Abstract |
Taltirelin (TAL) is a thyrotropin-releasing hormone (TRH) analog that is approved for use in humans in Japan. In this study, we characterized TAL binding to and signaling by the human TRH receptor (TRH-R) in a model cell system. We found that TAL exhibited lower binding affinities than TRH and lower signaling potency via the inositol-1,4,5-trisphosphate/calcium pathway than TRH. However, TAL exhibited higher intrinsic efficacy than TRH in stimulating inositol-1,4,5-trisphosphate second messenger generation. This is the first study that elucidates the pharmacology of TAL at TRH-R and shows that TAL is a superagonist at TRH-R. We suggest the superagonism exhibited by TAL may in part explain its higher activity in mediating central nervous system effects in humans compared to TRH. |
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