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

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 illustra...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-06, Vol.15 (11), p.2758-2760
Main Authors: Mustafa, Suni M, Bavadekar, Supriya A, Ma, Guoyi, Moore, Bob M, Feller, Dennis R, Miller, Duane D
Format: Article
Language:English
Subjects:
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
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0960-894X