Mechanisms underlying combined action of clonidine and local anesthetics.
We studied the mechanisms of combined action of clonidine and local anesthetics amethocaine and imidazo-benzimidazole derivative RU-1117. In contrast to amethocaine, RU-1117 in therapeutic concentrations binds to imidazoline receptors and, to a lesser extent, to alpha(2A)-adrenoceptors on human platelets. Clonidine and RU-1117 produce opposite effects on platelet aggregation induced by ADP in low concentrations. Our results suggest that the pharmacodynamic interaction of clonidine and RU-1117 is associated with their ability to activate the imidazolinergic system.
Ponomarev
V P
VP
Krasnodar Research Center, Russian Academy of Medical Sciences, Krasnodar Krai Administration, Moscow. ks@kmivc.ru
Galenko-Yaroshevskii
A P
AP
Dukhanin
A S
AS
Anisimova
V A
VA
D000244:Adenosine Diphosphate / Q000378:metabolism; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D000779:Anesthetics, Local / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D003000:Clonidine / Q000494:pharmacology*; D006801:Humans; D054755:Imidazoline Receptors; D020128:Inhibitory Concentration 50; D010974:Platelet Aggregation / Q000187:drug effects; D011485:Protein Binding; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism; D011955:Receptors, Drug / Q000737:chemistry; D013748:Tetracaine / Q000494:pharmacology; D013997:Time Factors
D000316:Adrenergic alpha-Agonists; D000779:Anesthetics, Local; D001562:Benzimidazoles; D054755:Imidazoline Receptors; C492532:RU-1117; D018341:Receptors, Adrenergic, alpha-2; D011955:Receptors, Drug; D013748:Tetracaine; D000244:Adenosine Diphosphate; D003000:Clonidine