Taltirelin

Drugbox
IUPAC_name = (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


CAS_number = 103300-74-9
CAS_supplemental = 201677-75-0
ATC_prefix =
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PubChem = 656609
DrugBank =
chemical_formula =
C=17 | H=31 | N=7 | O=9
molecular_weight = 477.46 g/mol
smiles = CN1C(=O)C [C@H] (NC1=O)C(=O)N [C@@H] (CC2=CN=CN2)C(=O)N3CCC [C@H] 3C(=O)N
bioavailability =
protein_bound =
metabolism =
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pregnancy_US =
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routes_of_administration = 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,cite journal |author=Fukuchi I, Asahi T, Kawashima K, "et al" |title=Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain |journal=Arzneimittelforschung |volume=48 |issue=4 |pages=353–9 |year=1998 |month=April |pmid=9608876 |doi= |url=] and little development of tolerance following prolonged dosing. [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] It has nootropic, [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] neuroprotective [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] and analgesic effects, [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] and is primarily being researched for the treatment of Spinocerebellar ataxia.

References

* [http://di.mt-pharma.co.jp/file/dc/cdt.pdf Ceredist セレジスト錠] (PDF) Mitsubishi Tanabe Pharma. October 2007.

External links

* [http://www.mt-pharma.co.jp Official Mitsubishi Tanabe Pharma Website]


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