名前:タルチレリン
ほかの名前: あたり 0910;タルチレリン;タルティレリン;セレディスト, あたり-0910;酢酸タルチレリン;あたり-0910, タルチレリン;タルチレリン中間体;タルチレリン中間体;酢酸タルチレリン,あたり-0910;L-プロリンアミド,(4S)-ヘキサヒドロ-1-メチル-
分子式: C17H23N7O5
分子量: 405.41
カス番号: 103300-74-9
純度:98%
外観: 白い粉
ソース: 合成
タルチレリン (marketed under the tradename Ceredist) is a thyrotropin-releasing hormone (TRH) analog, which mimics the physiological actions of TRH, but with a much longer half-life and duration of effects,and little development of tolerance following prolonged dosing.It has nootropic,neuroprotective and analgesic effects.
Taltirelin is primarily being researched for the treatment of spinocerebellar ataxia; limited research has also been carried out with regard to other neurodegenerative disorders
タルチレリン (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.
