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Matches in SemOpenAlex for { <https://semopenalex.org/work/W2088844744> ?p ?o ?g. }

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• W2088844744 abstract "We report the synthesis and evaluation of novel α1a adrenoceptor subtype-selective antagonists. Systematic modification of the lipophilic 4,4-diphenylpiperidinyl moiety of the dihydropyridine derivatives 1 and 2 provided several highly selective and potent α1a antagonists. From this series, we identified the 4-(methoxycarbonyl)-4-phenylpiperidine analogue SNAP 5540 (−) [(−)-63] for further characterization. When examined in an isolated human prostate tissue assay, this compound was found to have a Ki of 2.8 nM, in agreement with the cloned human receptor binding data (Ki = 2.42 nM). Further evaluation of the compound in isolated dog prostate tissue showed a Ki of 3.6 nM and confirmed it to be a potent antagonist (Kb = 1.6 nM). In vivo, this compound effectively blocked the phenylephrine-stimulated increase in intraurethral pressure (IUP) in mongrel dogs, at doses which did not significantly affect the arterial pressure (diastolic blood pressure, DBP), with a DBP Kb/IUP Kb ratio of 16. In addition, (−)-63 also showed greater than 40 000-fold selectivity over the rat L-type calcium channel and 200-fold selectivity over several G protein-coupled receptors, including histamine and serotonin subtypes. These findings prove that α1a adrenoceptor-subtype selective antagonists such as (−)-63 may be developed as uroselective agents for an improved treatment of BPH over nonselective α1 antagonists such as prazosin and terazosin, with fewer side effects." @default.
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• W2088844744 date "1998-11-20" @default.
• W2088844744 modified "2023-10-11" @default.
• W2088844744 title "Design and Synthesis of Novel α_1a Adrenoceptor-Selective Dihydropyridine Antagonists for the Treatment of Benign Prostatic Hyperplasia" @default.
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• W2088844744 doi "https://doi.org/10.1021/jm980506g" @default.
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• W2088844744 hasPublicationYear "1998" @default.
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