Abstract
The synthesis and biological activity of a series of benzofuro[3,2-c]pyridines and a benzothieno[3,2-c]pyridine are described. These compounds exhibit high affinity for the alpha 2-adrenoceptor, with high selectivity versus the alpha 1-receptor. Compound 1 also shows potent in vivo central activity and has been selected for further biological and clinical evaluation.
MeSH terms
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Adrenergic alpha-Agonists / metabolism
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Adrenergic alpha-Agonists / pharmacology
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / metabolism
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Adrenergic alpha-Antagonists / pharmacology*
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Animals
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Antidepressive Agents / chemical synthesis*
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Antidepressive Agents / metabolism
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Antidepressive Agents / pharmacology*
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CHO Cells
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Clonidine / metabolism
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Clonidine / pharmacology
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Cricetinae
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Humans
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Male
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Prazosin / metabolism
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Prazosin / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / metabolism
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Pyridines / pharmacology*
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Radioligand Assay
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Rats
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Receptors, Adrenergic, alpha-2 / metabolism*
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Xylazine / metabolism
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Xylazine / pharmacology
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Yohimbine / metabolism
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Yohimbine / pharmacology
Substances
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Adrenergic alpha-Agonists
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Adrenergic alpha-Antagonists
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Antidepressive Agents
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Pyridines
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Receptors, Adrenergic, alpha-2
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Xylazine
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Yohimbine
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Clonidine
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Prazosin