Abstract
A series of high affinity CRF receptor ligands with an imidazo[4,5-c]pyridine core is described. Individual analogues were synthesized and tested in vitro in rat brain receptors to determine binding affinity. The best compound was further tested in the dog N-in-1 pharmacokinetic model to assess oral bioavailability at 1 mg/kg po.
MeSH terms
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Administration, Oral
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Animals
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Anti-Anxiety Agents / chemical synthesis
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Anti-Anxiety Agents / metabolism
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Anti-Anxiety Agents / pharmacology*
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Anxiety Disorders / drug therapy
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Biological Availability
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Dogs
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Ligands
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Pyridines / chemical synthesis
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Pyridines / metabolism
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Pyridines / pharmacology*
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Rats
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Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors
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Receptors, Corticotropin-Releasing Hormone / metabolism*
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Structure-Activity Relationship
Substances
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Anti-Anxiety Agents
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Ligands
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Pyridines
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Receptors, Corticotropin-Releasing Hormone