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Title: Searching for new uroselective α1 – adrenergic receptor antagonist in the group pf arylosulfonamide derivatives of aryloxyalkilamines
Abstract:
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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Last modified:
Mar 13, 2023
In our library since:
Jun 18, 2020
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12
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http://dl.cm-uj.krakow.pl:8080/publication/4332
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| Edition name | Date |
|---|---|
| ZB-131399 | Mar 13, 2023 |
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