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Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 1999 Jul 19; Vol. 9 (14), pp. 1895-900. - Publication Year :
- 1999
-
Abstract
- Rational drug design utilizing a receptor homology model of the human muscarinic M1 receptor led to the discovery of the highly potent (Ki = 2 nM), efficacious, and in vivo functionally-selective M1 agonist, WAY-132983.
- Subjects :
- Administration, Oral
Animals
CHO Cells metabolism
Carbachol chemistry
Carbachol metabolism
Carbachol pharmacology
Cerebral Cortex metabolism
Cognition Disorders drug therapy
Computer Simulation
Cricetinae
Crystallography, X-Ray
Drug Design
Drug Evaluation, Preclinical
Humans
Macaca mulatta
Maze Learning drug effects
Models, Molecular
Phosphatidylinositols metabolism
Protein Conformation
Pyridines chemistry
Pyridines pharmacology
Rats
Receptor, Muscarinic M1
Receptors, Muscarinic chemistry
Salivation drug effects
Structure-Activity Relationship
Thiadiazoles chemistry
Thiadiazoles pharmacology
Bridged-Ring Compounds chemistry
Bridged-Ring Compounds pharmacology
Muscarinic Agonists chemistry
Muscarinic Agonists pharmacology
Pyrazines chemistry
Pyrazines pharmacology
Receptors, Muscarinic metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 9
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 10450949
- Full Text :
- https://doi.org/10.1016/s0960-894x(99)00313-3