Taltirelin
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Taltirelin ??
- ???
- 72-75°
- ??
- 25D -13.6° (c = 1 in water)
- ??
- 1.447±0.06 g/cm3(Predicted)
- ?? ??
- Store at +4°C
- ??? ??
- Solid
- ?? ?? (pKa)
- 9.32±0.40(Predicted)
- ??
- White to off-white
- ???
- Soluble to 50 mM in sterile water
- InChIKey
- PGQRTQMGGUFKCM-DLOVCJGASA-N
- SMILES
- C(N)(=O)[C@@H]1CCCN1C(=O)[C@H](C[C@@H]1NCNC1)NC(C1=CC(=O)N(C)C(=O)N1)=O
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Taltirelin C??? ??, ??, ??
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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.??
Taltirelin is a thyrotropin-releasing hormone analog.???? ??
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 ?? ?? ? ???
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Taltirelin ?? ??
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