Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Structure–activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-10, Vol.15 (20), p.4589-4593
Hauptverfasser:	Chua, Peter C., Nagasawa, Johnny Y., Bleicher, Leo S., Munoz, Benito, Schweiger, Edwin J., Tehrani, Lida, Anderson, Jeffrey J., Cramer, Merryl, Chung, Janice, Green, Mitchell D., King, Chris D., Reyes-Manalo, Grace, Cosford, Nicholas D.P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonist Biological and medical sciences CNS Excitatory Amino Acid Antagonists - pharmacokinetics Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences mGlu5 Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyridines - pharmacokinetics Pyridines - pharmacology Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	Structure–activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.06.099