Taltirelin

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,[1] and little development of tolerance following prolonged dosing.[2] It has nootropic,[3] neuroprotective[4] and analgesic effects.[5]

Taltirelin
Clinical data
Other names(4S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(3H-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
  • none
Identifiers
  • N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H31N7O9
Molar mass477.475 g·mol−1
3D model (JSmol)
  • CN1C(=O)C[C@H](NC1=O)C(=O)N[C@@H](CC2=CN=CN2)C(=O)N3CCC[C@H]3C(=O)N
  • 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 ☒N
  • Key:LQZAIAZUDWIVPM-SRVKXCTJSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Taltirelin is primarily being researched for the treatment of spinocerebellar ataxia; limited research has also been carried out with regard to other neurodegenerative disorders, e.g., spinal muscular atrophy.[6][7][8]

References
  1. Fukuchi I, Asahi T, Kawashima K, Kawashima Y, Yamamura M, Matsuoka Y, Kinoshita K (April 1998). "Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain". Arzneimittel-Forschung. 48 (4): 353–9. PMID 9608876.
  2. Asai H, Asahi T, Yamamura M, Yamauchi-Kohno R, Saito A (December 2005). "Lack of behavioral tolerance by repeated treatment with taltirelin hydrate, a thyrotropin-releasing hormone analog, in rats". Pharmacology, Biochemistry, and Behavior. 82 (4): 646–51. doi:10.1016/j.pbb.2005.11.004. PMID 16368129. S2CID 29935657.
  3. Yamamura M, Suzuki M, Matsumoto K (October 1997). "[Synthesis and pharmacological action of TRH analog peptide (Taltirelin)]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica. 110 Suppl 1: 33P–38P. doi:10.1254/fpj.110.supplement_33. PMID 9503402.
  4. Urayama A, Yamada S, Kimura R, Zhang J, Watanabe Y (December 2002). "Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice". Life Sciences. 72 (4–5): 601–7. doi:10.1016/S0024-3205(02)02268-3. PMID 12467901.
  5. Tanabe M, Tokuda Y, Takasu K, Ono K, Honda M, Ono H (February 2007). "The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems". British Journal of Pharmacology. 150 (4): 403–14. doi:10.1038/sj.bjp.0707125. PMC 2189720. PMID 17220907.
  6. Takeuchi Y, Miyanomae Y, Komatsu H, Oomizono Y, Nishimura A, Okano S, et al. (July 1994). "Efficacy of thyrotropin-releasing hormone in the treatment of spinal muscular atrophy". Journal of Child Neurology. 9 (3): 287–9. doi:10.1177/088307389400900313. PMID 7930408. S2CID 41678161.
  7. Tzeng AC, Cheng J, Fryczynski H, Niranjan V, Stitik T, Sial A, et al. (2000). "A study of thyrotropin-releasing hormone for the treatment of spinal muscular atrophy: a preliminary report". American Journal of Physical Medicine & Rehabilitation. 79 (5): 435–40. doi:10.1097/00002060-200009000-00005. PMID 10994885. S2CID 20416253.
  8. Kato Z, Okuda M, Okumura Y, Arai T, Teramoto T, Nishimura M, et al. (August 2009). "Oral administration of the thyrotropin-releasing hormone (TRH) analogue, taltireline hydrate, in spinal muscular atrophy". Journal of Child Neurology. 24 (8): 1010–2. doi:10.1177/0883073809333535. PMID 19666885. S2CID 29321906.


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