Chemistry:Taltirelin

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Short description: Chemical compound
Taltirelin
Talitirelin.png
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
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
Chemical and physical data
FormulaC17H31N7O9
Molar mass477.475 g·mol−1
3D model (JSmol)
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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 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. "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. April 1998. PMID 9608876. 
  2. "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. December 2005. doi:10.1016/j.pbb.2005.11.004. PMID 16368129. 
  3. "[Synthesis and pharmacological action of TRH analog peptide (Taltirelin)]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 110 Suppl 1: 33P–38P. October 1997. doi:10.1254/fpj.110.supplement_33. PMID 9503402. 
  4. "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. December 2002. doi:10.1016/S0024-3205(02)02268-3. PMID 12467901. 
  5. "The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems". British Journal of Pharmacology 150 (4): 403–14. February 2007. doi:10.1038/sj.bjp.0707125. PMID 17220907. 
  6. "Efficacy of thyrotropin-releasing hormone in the treatment of spinal muscular atrophy". Journal of Child Neurology 9 (3): 287–9. July 1994. doi:10.1177/088307389400900313. PMID 7930408. 
  7. "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. 2000. doi:10.1097/00002060-200009000-00005. PMID 10994885. 
  8. "Oral administration of the thyrotropin-releasing hormone (TRH) analogue, taltireline hydrate, in spinal muscular atrophy". Journal of Child Neurology 24 (8): 1010–2. August 2009. doi:10.1177/0883073809333535. PMID 19666885. 

External links