taltirelin

Description: Taltirelin (TA-0910; tradename Ceredist) is a thyrotropin-releasing hormone (TRH) analog and a TRH mimic that acts as a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release). Taltirelin alleviates mechanical allodynia through activation of descending monoaminergic neurons in persistent inflammatory pain. Compare to TRH, it has a much longer half-life and duration of effects, andlittle development of tolerance following prolonged dosing. It hasnootropic, neuroprotective and analgesic effects

References:

1. ThirunarayananN, et al. Taltirelin is a superagonist at the humanthyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne).2012 Oct 9; 3:120.

2. Eto K, Kim SK, Nabekura J, Ishibashi H. Taltirelin, a thyrotropin-releasing hormone analog, alleviates mechanical allodynia through activation of descending monoaminergic neurons in persistent inflammatory pain. Brain Res. 2011 Sep 26; 1414:50-7. doi: 10.1016/j.brainres.2011.07.065. Epub 2011 Aug 6. PubMed PMID: 21872219.