| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H23N7O5 |
| Molecular Weight | 405.4084 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)C[C@H](NC1=O)C(=O)N[C@@H](CC2=CN=CN2)C(=O)N3CCC[C@H]3C(N)=O
InChI
InChIKey=LQZAIAZUDWIVPM-SRVKXCTJSA-N
InChI=1S/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1
| Molecular Formula | C17H23N7O5 |
| Molecular Weight | 405.4084 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Taltirelin (TA-0910), a synthetic thyrotropin-releasing hormone (TRH) analog, has been developed by Tanabe Seiyaku for the treatment of neurodegenerative diseases. Taltirelin mimics the physiological actions of TRH, but with a much longer half-life and duration of effects, and little development of tolerance following prolonged dosing. Taltirelin has nootropic, neuroprotective and analgesic effects. 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.
CNS Activity
Originator
Approval Year
Doses
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
PubMed
Patents
Sample Use Guides
Patients took taltirelin (5 mg bid) or placebo for 28 to 52 weeks.
Route of Administration:
Oral
HEK-EM 293 (human embryonic kidney) cells stably expressing TRH-R were seeded in black-walled, clear bottomed 96-well plates (Corning, NY, USA) at a density of 60,000 cells/well in DMEM with 10% fetal bovine serum and incubatedfor24hat37◦C in5%CO2. The following day, the culture media was replaced with 100 μl of Hank’s balanced salt solution with 20 mM HEPES, pH 7.5 and the cells were loaded with100 μl of calcium 4 fluorescent dye (Molecular Devices, Sunnyvale, CA, USA) for 1 h at room temperature before addition of compounds .Transient changes in intracellular [Ca++] induced by TALTIRELIN were measured using the FLIPRTETRA system (Molecular Devices, Sunnyvale, CA, USA). Changes in fluorescence were detected at the emission wavelength ranges from 515 to 575 nm. The agonistic responses of ligands were assessed immediately upon their addition in a concentration range from 0.1 nMto30 μM.
