Taltirelin

Bezeichnung:Taltirelin

CAS-Nr103300-74-9

Englisch Name:Taltirelin

CBNumberCB31177191

SummenformelC17H23N7O5

Molgewicht405.41

MOL-Datei103300-74-9.mol

Taltirelin physikalisch-chemischer Eigenschaften

Schmelzpunkt	72-75°
alpha	25D -13.6° (c = 1 in water)
Dichte	1.447±0.06 g/cm3(Predicted)
storage temp.	Store at +4°C
Aggregatzustand	Solid
pka	9.32±0.40(Predicted)
Farbe	White to off-white
Wasserlöslichkeit	Soluble to 50 mM in sterile water

Taltirelin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Taltirelin was marketed in Japan for the treatment of neurodegenerative diseases, in particular the improvement of ataxia due to spino-cerebellar degeneration (SCD); it is the first orally-active drug in this indication. This synthetic thyrotropin-releasing hormone (TRH) analog is prepared by condensation of (S)-1-methyl-4,5-dihydroorotic acid with L-histidyl-Lprolinamide. It was shown that the S-configuration for all 3 chiral centers is crucial for CNS activity. Taltirelin is a potent agonist of the TRH receptors that shows significant effects on the cerebral monoamine systems when administered i.p. in rats. As TRH at 10-fold higher doses, taltirelin has been found to increase the extracellular levels of dopamine and its metabolites (DOPAC and HVA) as well as precursors and/or metabolites of noradrenaline and serotonin in different areas of the rat brain. Taltirelin produced an anti-ataxic activity in the Rolling mouse Nagoya, an ataxic mutant mouse. In several clinical studies performed in patients suffering from various forms of SCD, taltirelin demonstrated a statistically significant increase in the global improvement of ataxic symptoms and other neurologic abnormalities.
Originator
Tanabe Seiyaku (Japan)
Verwenden
Taltirelin is a thyrotropin-releasing hormone analog.
Verwenden
Analog of thyrotropin releasing hormone TRH, with pronounced CNS activity. Used in the treatment of spinocerebellar degeneration.
Definition
ChEBI: Taltirelin is an oligopeptide comprising of (4S)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxylic acid, L-histidine and L-prolinamide joined in sequence by peptide linkages. It is a thyrotropin-releasing hormone (TRH) analog. Its tetrahydrate form is approved in Japan for the treatment of spinal muscular atrophy. It has a role as a nootropic agent, a neuroprotective agent and an analgesic.
Trademarks
Ceredist
Biologische Aktivität
Synthetic thyrotropin-releasing hormone (TRH) analog. Displays ~ 30-100-fold more potent CNS activity and ~ 50-fold weaker endocrine activity than TRH. Antinociceptive and neuroprotective.

Taltirelin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

103300-74-9, Taltirelin Verwandte Suche:

Send Inquriy