Yohimbine dimers exhibiting binding selectivities for human α 2a - versus α 2b -adrenergic receptors

Bioorganic & Medicinal Chemistry Letters
2000.0

Abstract

A series of yohimbine dimers was prepared and evaluated at the human alpha2a- and alpha2b-adrenergic receptors (ARs) expressed in Chinese hamster ovary (CHO) cells. All dimers display higher binding selectivities for alpha2a versus alpha2b subtype than yohimbine, and four compounds (3d, 3e, 3g and 3i) represent the most potent and alpha2a versus alpha2b-AR selective ligands identified so far.

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