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Title: Searching for new uroselective α1 – adrenergic receptor antagonist in the group pf arylosulfonamide derivatives of aryloxyalkilamines


The aim of the study was to select from among 43 arylsulfonamide derivatives of (aryloxy) alkylamines, uroselective structures with the highest preference for subtypes A and D of α1-adrenoceptor (AR), which would provide the basis for further studies of these compounds as candidates in the treatment of prostatic hyperplasia.Pharmacological screening included the determination of α1- and α2-AR affinities and intrinsic activity for α1A and α1B -AR. Four structures were identified: PZ - 962, PZ - 1204, PZ - 1205 and PZ - 1206, which were passed on to further research, including the determination of intrinsic activity for α1D-AR and antagonistic activity against α1A, α1B and α1D-AR in biofunctional studies. Subsequently, hypotensive activity after single iv. and chronic ip. administration in rats, the effects on pressure activity elicited by methoxamine, plasma carbohydrate-lipid profile, normal rat electrocardiogram and cholinolytic activity were evaluated.Finally, there were identified structures with significant α1-adrenolytic activity and beneficial influence on lipid-carbohydrate parameters, demonstrating no relevant effects on cardio-vascular system. Selected compounds showed no higher binding preference for α1A/D-AR than tamsulosin, neither cholinolytic activity. Although weaker receptor activity of selected compounds was found in comparison to tamsulosin, the final confirma ; tion of effectiveness in alleviating BPH symptoms will be carrying out by urodynamic studies in an animal model.

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2 - studia doktoranckie

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Wydział Farmaceutyczny


Sapa, Jacek

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Mar 13, 2023

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Jun 18, 2020

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ZB-131399 Mar 13, 2023


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