Experimental approach to differentiation of the effects mediated by imidazole receptors and alpha2-adrenoceptors on platelets.
We studied parameters of specific binding for various ligands of imidazole receptors and alpha2-adrenoceptors on human platelets. Pharmacological activity of compounds was evaluated by their effects on platelet aggregation induced by ADP in low concentrations (0.125-1.5 microM). In contrast to alpha2-adrenoceptor agonist norepinephrine inducing reversible aggregation of cells, selective stimulation of imidazole receptors with moxonidine produced a disaggregation effect. The data suggest that human platelets can be used as an experimental test system for screening and study of molecular mechanisms underlying the influence of new compounds.
Ponomarev
V V
VV
Krasnodar Research Center, Russian Academy of Medical Sciences, Krasnodar Krai Administration, Moscow.
Galenko-Yaroshevskii
A P
AP
Dukhanin
A S
AS
D000244:Adenosine Diphosphate / Q000378:metabolism; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D003000:Clonidine / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000378:metabolism* / Q000494:pharmacology; D008024:Ligands; D009638:Norepinephrine / Q000494:pharmacology; D010974:Platelet Aggregation / Q000502:physiology; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism*; D011955:Receptors, Drug / Q000378:metabolism*
D000316:Adrenergic alpha-Agonists; D007093:Imidazoles; D008024:Ligands; D010975:Platelet Aggregation Inhibitors; D018341:Receptors, Adrenergic, alpha-2; D011955:Receptors, Drug; D000244:Adenosine Diphosphate; C029899:imidazole; C043482:moxonidine; D003000:Clonidine; D009638:Norepinephrine