New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.

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Kennis LE, Bischoff FP, Mertens CJ, Love CJ, Van den Keybus FA, Pieters S, Braeken M, Megens AA, Leysen JE

New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):71-4.

PubMed ID
10636247 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MirtazapineAlpha-2A adrenergic receptorIC 50 (nM)85.11N/AN/ADetails