Taltirelin

Taltirelin
Systematic (IUPAC) name
N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide
Clinical data
AHFS/Drugs.com International Drug Names
Routes of
administration		 Oral
Identifiers
CAS Number 103300-74-9 YesY
201677-75-0
ATC code none
PubChem CID 656609
IUPHAR/BPS 2143
ChemSpider 102734 N
UNII DOZ62MV6A5 YesY
Synonyms (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
Chemical data
Formula C17H31N7O9
Molar mass 477.46 g/mol
 NYesY (what is this?)  (verify)

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. ↑ Fukuchi, I.; Asahi, T.; Kawashima, K.; Kawashima, Y.; Yamamura, M.; Matsuoka, Y.; Kinoshita, K. (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): 353–359. PMID 9608876.
  2. ↑ Asai, H.; Asahi, T.; Yamamura, M.; Yamauchi-Kohno, R.; Saito, A. (2005). "Lack of behavioral tolerance by repeated treatment with taltirelin hydrate, a thyrotropin-releasing hormone analog, in rats". Pharmacology Biochemistry and Behavior 82 (4): 646–651. doi:10.1016/j.pbb.2005.11.004. PMID 16368129.
  3. ↑ Yamamura, M.; Suzuki, M.; Matsumoto, K. (1997). "Synthesis and pharmacological action of TRH analog peptide (Taltirelin)". Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 110 Suppl 1: 33P–38P. PMID 9503402.
  4. ↑ Urayama, A.; Yamada, S.; Kimura, R.; Zhang, J.; Watanabe, Y. (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): 601–607. doi:10.1016/S0024-3205(02)02268-3. PMID 12467901.
  5. ↑ Tanabe, M.; Tokuda, Y.; Takasu, K.; Ono, K.; Honda, M.; Ono, H. (2009). "The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems". British Journal of Pharmacology 150 (4): 403–414. doi:10.1038/sj.bjp.0707125. PMC 2189720. PMID 17220907.
  6. ↑ Takeuchi, Y.; Miyanomae, Y.; Komatsu, H.; Oomizono, Y.; Nishimura, A.; Okano, S.; Nishiki, T.; Sawada, T. (1994). "Efficacy of Thyrotropin-Releasing Hormone in the Treatment of Spinal Muscular Atrophy". Journal of Child Neurology 9 (3): 287–289. doi:10.1177/088307389400900313. PMID 7930408.
  7. ↑ Tzeng, A. C.; Cheng, J.; Fryczynski, H.; Niranjan, V.; Stitik, T.; Sial, A.; Takeuchi, Y.; Foye, P.; Deprince, M.; Bach, J. R. (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): 435–440. doi:10.1097/00002060-200009000-00005. PMID 10994885.
  8. ↑ Kato, Z.; Okuda, M.; Okumura, Y.; Arai, T.; Teramoto, T.; Nishimura, M.; Kaneko, H.; Kondo, N. (2009). "Oral Administration of the Thyrotropin-Releasing Hormone (TRH) Analogue, Taltireline Hydrate, in Spinal Muscular Atrophy". Journal of Child Neurology 24 (8): 1010–1012. doi:10.1177/0883073809333535. PMID 19666885.

External links


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