Structure–activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Studies of structure–activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data. Studies of structure–activity relationships for the linker in a new series of metabotropic glutamate rece...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-09, Vol.16 (18), p.4788-4791
Main Authors: Bach, Peter, Nilsson, Karolina, Svensson, Tor, Bauer, Udo, Hammerland, Lance G., Peterson, Alecia, Wållberg, Andreas, Österlund, Krister, Karis, David, Boije, Maria, Wensbo, David
Format: Article
Language:English
Subjects:
Alkynes - chemical synthesis
Alkynes - chemistry
Alkynes - pharmacokinetics
Alkynes - pharmacology
Animals
Biological and medical sciences
Cross-Linking Reagents - chemistry
Digestive system
Gastro-esophageal reflux disease (GERD)
Glutamatergic system (aspartate and other excitatory aminoacids)
Liver - drug effects
Liver - metabolism
Medical sciences
mGluR5 antagonists
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Pyridines - chemistry
Pyridinyl-alkynes
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate - antagonists & inhibitors
Receptors, Metabotropic Glutamate - metabolism
SAR
Structure-Activity Relationship
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Summary:Studies of structure–activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data. Studies of structure–activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.06.078