| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H22N2O2 |
| Molecular Weight | 382.4544 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC[C@H](NC(=O)C1=C(O)C(=NC2=C1C=CC=C2)C3=CC=CC=C3)C4=CC=CC=C4
InChI
InChIKey=BIAVGWDGIJKWRM-FQEVSTJZSA-N
InChI=1S/C25H22N2O2/c1-2-20(17-11-5-3-6-12-17)27-25(29)22-19-15-9-10-16-21(19)26-23(24(22)28)18-13-7-4-8-14-18/h3-16,20,28H,2H2,1H3,(H,27,29)/t20-/m0/s1
| Molecular Formula | C25H22N2O2 |
| Molecular Weight | 382.4544 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Talnetant (SB-223412) is a selective, orally active neurokinin 3 receptor antagonist and is under development for the potential treatment of several disorders, including irritable bowel syndrome, schizophrenia, chronic obstructive pulmonary disease, cough, overactive bladder and urinary incontinence. The most common adverse effects were headache, fatigue, and nausea.
CNS Activity
Originator
Approval Year
Doses
Sourcing
Sample Use Guides
0.1 mg to 1000 mg as single doses; up to 800 mg twice daily on repeat doses.
Route of Administration:
Oral
SB223412 antagonized senktide-induced contraction of rabbit isolated iris sphincter muscle (KB = 1.6 nM), and inhibited NK-3 receptorinduced
membrane depolarization in guinea-pig bronchial parasympathetic ganglia and substantia nigra pars compacta in guinea pig.
SB223412 inhibited senktide-induced miosis in rabbits when given iv (ED50 = 0.44mg/kg) and by 53% when given orally (25 mg/kg, PO).
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TARGET -> INHIBITOR |
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SALT/SOLVATE -> PARENT |
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