[Effect of the chronic use of propranolol on the specific binding of 3H-WB-4101 with the membranes of the mesenteric vessels in rats].
It has been shown that the 15-bay use of dl-propranolol (100 mg/kg a day) leads to a significant increase in the dissociation constant (CD) of the sites of specific binding of 3H-WB-4101 with membranes of rat mesenteric vessels. The concentration (Bmax) of the binding sites does not significantly change. Propranolol and other adrenoblockers do not possess any affinity for alpha-adrenoreceptors of rat brain synaptic membranes, i.e. changes in the properties of these receptors in vascular membranes cannot be accounted for by the direct action of propranolol in vivo or by the influence of the drug left in the membranes in vitro. It is concluded that desensitization of alpha1-adrenoreceptors of the peripheral vessels may be an essential element in the mechanism of the hypotensive action under the chronic use of beta-adrenoblockers.
Ismailov
Sh I
ShI
Rozhanets
V V
VV
Val'dman
A V
AV
D000317:Adrenergic alpha-Antagonists / Q000378:metabolism*; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D004146:Dioxanes / Q000378:metabolism*; D004147:Dioxins / Q000378:metabolism*; D008297:Male; D008638:Mesenteric Arteries / Q000187:drug effects* / Q000378:metabolism; D008642:Mesenteric Veins / Q000187:drug effects* / Q000378:metabolism; D011433:Propranolol / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects* / Q000378:metabolism; D013570:Synaptic Membranes / Q000187:drug effects / Q000378:metabolism; D013997:Time Factors; D014316:Tritium
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D004146:Dioxanes; D004147:Dioxins; D011942:Receptors, Adrenergic, alpha; D014316:Tritium; D011433:Propranolol; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane
Vliianie khronicheskogo primeneniia proprapolola na spetsificheskoe sviazyvanie 3H-WB-4101 s membranami bryzheechnykh sosudov krys.