Taltirelin

• CAT Number: I000198
• CAS Number: 103300-74-9
• Molecular Formula: C17H23N7O5
• Molecular Weight: 405.41
• Purity: ≥95%
• Solubility: DMSO：≥ 32 mg/mL
• Storage: 3 years -20C powder
• InChI: 1S/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1
• InChIKey: LQZAIAZUDWIVPM-SRVKXCTJSA-N
• SMILES: C1[C@H](N(CC1)C([C@@H](NC([C@@H]1CC(N(C)C(=O)N1)=O)=O)Cc1cnc[nH]1)=O)C(N)=O

Taltirelin (CAT: I000198), also known as TA0910, is a novel orally active analog of thyrotropin-releasing hormone (TRH). It exhibits binding activity to TRH receptors in the brain of rats. TRH receptors are found in various regions of the brain and are involved in the regulation of several physiological processes, including the release of thyroid-stimulating hormone (TSH) and prolactin. Taltirelin has been studied for its potential therapeutic applications in conditions related to hypothalamic dysfunction, such as hypothyroidism and depression. Its binding affinity to TRH receptors suggests its ability to modulate the activity of these receptors and potentially influence related signaling pathways.

Reference

1: Dougherty JP, Wolff BS, Cullen MJ, Saligan LN, Gershengorn MC. Taltirelin
alleviates fatigue-like behavior in mouse models of cancer-related fatigue.
Pharmacol Res. 2017 Oct;124:1-8. doi: 10.1016/j.phrs.2017.07.012. Epub 2017 Jul
15. PubMed PMID: 28720519; PubMed Central PMCID: PMC5587390.

2: Thirunarayanan N, Nir EA, Raaka BM, Gershengorn MC. Thyrotropin-releasing
hormone receptor type 1 (TRH-R1), not TRH-R2, primarily mediates taltirelin
actions in the CNS of mice. Neuropsychopharmacology. 2013 May;38(6):950-6. doi:
10.1038/npp.2012.256. Epub 2012 Dec 11. PubMed PMID: 23303050; PubMed Central
PMCID: PMC3629383.

3: Thirunarayanan N, Raaka BM, Gershengorn MC. Taltirelin is a superagonist at
the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne).
2012 Oct 9;3:120. doi: 10.3389/fendo.2012.00120. eCollection 2012. PubMed PMID:
23087672; PubMed Central PMCID: PMC3466466.

4: 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.

5: Nakamura T, Honda M, Kimura S, Tanabe M, Oda S, Ono H. Taltirelin improves
motor ataxia independently of monoamine levels in rolling mouse nagoya, a model
of spinocerebellar atrophy. Biol Pharm Bull. 2005 Dec;28(12):2244-7. PubMed PMID:
16327158.

6: Fukuchi I, Asahi T, Kawashima K, Kawashima Y, Yamamura M, Matsuoka Y,
Kinoshita K. Effects of taltirelin hydrate (TA-0910), a novel
thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in
rat brain. Arzneimittelforschung. 1998 Apr;48(4):353-9. PubMed PMID: 9608876.