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Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence
- Source :
- Bioorganic & Medicinal Chemistry Letters. 21:3354-3357
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration.
- Subjects :
- Parenteral Nutrition
medicine.medical_specialty
Clinical Biochemistry
TRPV1
TRPV Cation Channels
Pharmaceutical Science
Urinary incontinence
Naphthols
Pharmacology
Biochemistry
Chemical synthesis
Inhibitory Concentration 50
Structure-Activity Relationship
chemistry.chemical_compound
Internal medicine
Drug Discovery
medicine
Animals
Phenol
Potency
Phenols
Receptor
Molecular Biology
Molecular Structure
medicine.diagnostic_test
Organic Chemistry
Cystometry
Rats
Disease Models, Animal
Urinary Incontinence
Endocrinology
chemistry
Molecular Medicine
Female
medicine.symptom
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....c525e2c652103e35eca7e52c0822cad3
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.04.013