Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors

Suni M Mustafa; Supriya A Bavadekar; Guoyi Ma; Bob M Moore; Dennis R Feller; Duane D Miller

doi:10.1016/j.bmcl.2005.03.116

Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2758-60. doi: 10.1016/j.bmcl.2005.03.116.

Authors

Suni M Mustafa¹, Supriya A Bavadekar, Guoyi Ma, Bob M Moore, Dennis R Feller, Duane D Miller

Affiliation

¹ Department of Pharmaceutical Sciences, University of Tennessee, Health Science Center, Memphis, 38163, USA.

PMID: 15911252
DOI: 10.1016/j.bmcl.2005.03.116

Abstract

A series of yohimbine derivatives was synthesized and evaluated for binding affinity at the human alpha(2C)-adrenergic receptors expressed in Chinese hamster ovary cells. It has been found that compound 5 shows a higher affinity for alpha(2C)-AR than the parent compound yohimbine 1, thereby illustrating that the nature of the linkers affect binding potencies on these receptors.

Publication types

Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

Animals
CHO Cells
Cricetinae
Humans
Mice
Protein Binding
Receptors, Adrenergic, alpha-2 / drug effects*
Receptors, Adrenergic, alpha-2 / metabolism
Yohimbine / chemical synthesis*
Yohimbine / metabolism
Yohimbine / pharmacology*

Substances

Receptors, Adrenergic, alpha-2
Yohimbine