Affinity of a 1,4-benzodioxane derivative with alpha-adrenolytic activity to isolated synaptic membranes from rat brain.
The experiments carried out with KS 5-2, dibozan and WB 4101 allowed for a comparison of the affinity of KS 5-2 with that of the other two compounds. High affinity of the three compounds and differences in their affinity with respect to the alpha-adrenergic receptors were established. The results were compared with the 1H-NMR spectroscopic data, revealing the intimate structure of WB 4101, dibozan and KS 5-2 in such a way as to substantiate their pharmacological action by their chemical structure.
Department of Pharmacology and Toxicology, Pharmaceutical Faculty, Medical Academy, Sofia, Bulgaria.
V
V
Spassov
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Danchev
D000317:Adrenergic alpha-Antagonists / Q000378:metabolism*; D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D004146:Dioxanes / Q000378:metabolism*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D010879:Piperazines / Q000378:metabolism*; D051381:Rats; D013570:Synaptic Membranes / Q000187:drug effects / Q000378:metabolism*
D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D010879:Piperazines; C075227:KS 5-2; C100216:dibozane; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane