TY - JOUR
T1 - Isolation and partial purification of a clonidine‐displacing endogenous brain substance
AU - ATLAS, Daphne
AU - BURSTEIN, Yigal
PY - 1984/10
Y1 - 1984/10
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0012020765&partnerID=8YFLogxK
U2 - 10.1111/j.1432-1033.1984.tb08462.x
DO - 10.1111/j.1432-1033.1984.tb08462.x
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C2 - 6092070
AN - SCOPUS:0012020765
SN - 0014-2956
VL - 144
SP - 287
EP - 293
JO - European Journal of Biochemistry
JF - European Journal of Biochemistry
IS - 2
ER -