| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H16BrF3N4O |
| Molecular Weight | 429.234 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)C1=CN=C(C=C1)N2CC[C@H](C2)NC(=O)NC3=CC=CC=C3Br
InChI
InChIKey=JYILLRHXRVTRSH-GFCCVEGCSA-N
InChI=1S/C17H16BrF3N4O/c18-13-3-1-2-4-14(13)24-16(26)23-12-7-8-25(10-12)15-6-5-11(9-22-15)17(19,20)21/h1-6,9,12H,7-8,10H2,(H2,23,24,26)/t12-/m1/s1
| Molecular Formula | C17H16BrF3N4O |
| Molecular Weight | 429.234 |
| 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 |
SB-705498 is a selective vanilloid receptor-1 (VR1/TRPV1) antagonist developed by GlaxoSmithKline. The drug was tested in phase II of clinical trials for the treatment of pain (dental, rectal, in migraine) and rhinitis/cough. The development of the drug has been terminated by unknown reason (SB-705498 is no longer in GSK pipeline).
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
Non Allergic Rhinitis: 12mg intra-nasal SB-705498 once daily. Chronic Cough: take 400 or 600mg orally.
Route of Administration:
Other
The pharmacological activity of SB-705498 was characterized on HEK293 cells expressing the human TRPV1, using fluorometric calcium imaging. The cells were treated with different concentrations (10(-5)-10(-10) M) of the drug for 1 min or with 1uM for 30 min. The IC50 for the inhibition of 20 nM capsaicin-induced responses was estimated as 46 nM.
