Desensitization of platelet alpha 2-adrenoceptors after short term infusions of adrenoceptor agonist in man.
The effect of intravenous infusion of catecholamines and related drugs on human platelet alpha 2-adrenoceptor number and function was investigated. Short (60-120 min) infusions of catecholamines with alpha 2 agonist activity in vivo produced attenuation of the platelet responses to adrenaline in vitro. This desensitization was specific for the adrenaline induced aggregatory response. The maximum number of [3H]yohimbine binding sites on platelets was not altered by adrenaline infusion. The ability of adrenaline to reduce platelet cyclic AMP levels was significantly reduced after the infusions. Acute infusions of alpha 2-adrenoceptor agonists may alter the coupling of the platelet alpha 2-adrenoceptor to adenylate cyclase.
Jones
C R
CR
Giembcyz
M
M
Hamilton
C A
CA
Rodger
I W
IW
Whyte
K
K
Deighton
N
N
Elliott
H L
HL
Reid
J L
JL
D000293:Adolescent; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D000328:Adult; D001792:Blood Platelets / Q000378:metabolism*; D001794:Blood Pressure / Q000187:drug effects; D002395:Catecholamines / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D000242:Cyclic AMP / Q000097:blood; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*
D000316:Adrenergic alpha-Agonists; D002395:Catecholamines; D011942:Receptors, Adrenergic, alpha; D000242:Cyclic AMP