Isolation and partial purification of a clonidine‐displacing endogenous brain substance

Daphne ATLAS*, Yigal BURSTEIN

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

149 Scopus citations

Abstract

A new compound, designated clonidine‐displacing substance (CDS), has been isolated from calf brain by ion‐exchange chromatography, zone electrophoresis and high‐performance liquid chromatography. CDS binds specifically to α2‐adrenergic receptors in rat brain and human platelet membranes, as measured in direct binding experiments using [3H]clonidine and [3H]yohimbine respectively. Unlike clonidine or other α2‐agonists, CDS does not affect basal levels of adenylate cyclase in human platelets at the highest concentrations obtainable. The apparent molecular mass of the compound is estimated to be 500 ± 50 Da, as determined by gel‐filtration chromatography on Sephadex G‐15. The new compound is thermostable, not affected by proteolytic enzymes, such as trypsin. chymotrypsin, pronase, papain and pyroglutamase, or by boiling in 0.2 M HCl for 5min. It does not bind to α1receptors in rat brain or to β‐adrenergic receptors in turkey erythrocytes, since it is unable to displace [3H]prazosin and [125I]cyanopindolol from α1 and β‐receptors respectively.

Original languageEnglish
Pages (from-to)287-293
Number of pages7
JournalEuropean Journal of Biochemistry
Volume144
Issue number2
DOIs
StatePublished - Oct 1984

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