Back to Search
Start Over
Imidazopyridines: a novel class of hNav1.7 channel blockers.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Mar 01; Vol. 18 (5), pp. 1696-701. Date of Electronic Publication: 2008 Jan 18. - Publication Year :
- 2008
-
Abstract
- A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNa(v)1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10mg/kg.
- Subjects :
- Analgesics chemistry
Analgesics pharmacology
Animals
Inflammation drug therapy
Molecular Structure
NAV1.7 Voltage-Gated Sodium Channel
Pain drug therapy
Rats
Sodium Channel Blockers pharmacokinetics
Structure-Activity Relationship
Pyridines chemistry
Pyridines pharmacology
Sodium Channel Blockers chemistry
Sodium Channel Blockers pharmacology
Sodium Channels metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18243692
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.01.047