Nome:Taltirelin
Outro nome: POR 0910;Taltirelin;Taltireline;Ceredista, POR-0910;Acetato de Taltirelina;POR-0910, taltirelina;Taltirelin intermediário;INTERMEDIÁRIOS DE TALTIRELIN;Acetato de Taltirelina,POR-0910;L-Prolinamida,(4S)-hexa-hidro-1-metil-
Fórmula molecular: C17H23N7O5
Peso molecular: 405.41
Nº do caso: 103300-74-9
Pureza:98%
Aparência: pó branco
Fonte: sintético
Taltirelin (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
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. No entanto, 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.
