Taltirelin manufacturers and suppliers in india

Taltirelin

CAS:: 103300-74-9

MF:: C17H23N7O5

MW:: 405.41

Suppliers by country/region

Company Type

Properties

Melting point:: 72-75°

alpha: 25D -13.6° (c = 1 in water)

Density: 1.447±0.06 g/cm3(Predicted)

storage temp.: Store at +4°C

form: Solid

pka: 9.32±0.40(Predicted)

color: White to off-white

Water Solubility: Soluble to 50 mM in sterile water

Safety Information

Use

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.