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Taltirelin
Systematic (IUPAC) name
N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}- L-histidyl-L-prolinamide
Identifiers
CAS number 103300-74-9
201677-75-0
ATC code none
PubChem 656609
Chemical data
Formula C 17H31N7O9  
Mol. mass 477.46 g/mol
SMILES eMolecules & PubChem
Synonyms (4S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(3 H-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

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] and is primarily being researched for the treatment of Spinocerebellar ataxia.

References

  1. ^ Fukuchi I, Asahi T, Kawashima K, et al. (April 1998). "Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain". Arzneimittelforschung 48 (4): 353–9. PMID 9608876.  
  2. ^ Asai H, Asahi T, Yamamura M, Yamauchi-Kohno R, Saito A. Lack of behavioral tolerance by repeated treatment with taltirelin hydrate, a thyrotropin-releasing hormone analog, in rats. Pharmacology, Biochemistry and Behaviour. 2005 Dec;82(4):646-51. PMID 16368129
  3. ^ Yamamura M, Suzuki M, Matsumoto K. Synthesis and pharmacological action of TRH analog peptide (Taltirelin). Nippon Yakurigaku Zasshi. (Japanese). 1997 Oct;110 Suppl 1:33P-38P. PMID 9503402
  4. ^ Urayama A, Yamada S, Kimura R, Zhang J, Watanabe Y. 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. 2002 Dec 20;72(4-5):601-7. PMID 12467901
  5. ^ Tanabe M, Tokuda Y, Takasu K, Ono K, Honda M, Ono H. The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems. British Journal of Pharmacology. 2007 Feb;150(4):403-14. PMID 17220907

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