Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.

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Zheng W, Lei L, Lalchandani S, Sun G, Feller DR, Miller DD

Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.

Bioorg Med Chem Lett. 2000 Apr 3;10(7):627-30.

PubMed ID

10762040 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Yohimbine	Alpha-2A adrenergic receptor	Ki (nM)	0.42	N/A	N/A	Details
Yohimbine	Alpha-2B adrenergic receptor	Ki (nM)	2.01	N/A	N/A	Details