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A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2006 Jun 29; Vol. 49 (13), pp. 3753-6. - Publication Year :
- 2006
-
Abstract
- Melanin-concentrating hormone receptor antagonists containing thieno- and a benzopyridazinone cores were designed and tested as potential anorectic agents. These ligands showed high affinity for the receptor, potent functional activity in vitro, and good oral bioavailabilty in rats. The thiophene analogue exhibited low iv clearance, long half-life, and high brain penetration. In obese rats, the thienopyridazinone demonstrated a dose-dependent reduction in feeding and body weight with doses between 1 and 10 mg kg-1.
- Subjects :
- Animals
Appetite Depressants pharmacokinetics
Appetite Depressants pharmacology
Biological Availability
Body Weight drug effects
Brain metabolism
Eating drug effects
Half-Life
Male
Obesity drug therapy
Permeability
Pyridazines chemistry
Pyridazines pharmacology
Rats
Rats, Sprague-Dawley
Stereoisomerism
Structure-Activity Relationship
Thiophenes pharmacokinetics
Thiophenes pharmacology
Appetite Depressants chemical synthesis
Pyridazines chemical synthesis
Receptors, Somatostatin antagonists & inhibitors
Thiophenes chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 49
- Issue :
- 13
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 16789729
- Full Text :
- https://doi.org/10.1021/jm051263c