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PHARMACOLOGICAL EVALUATION OF PYRROLIDINES AS POTENT ! 1 - ADRENERGIC RECEPTOR ANTAGONIST WITH URO-SELECTIVE PROFILE

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Sapa J., Bednarski M., Nowiński L., Kotańska M., Knutelska J., Zaręba P., LECHOCKA-NOWAK A., BELCZYK M., ZYGMUNT M.

Medicina Internacia Revuo

2018

vol. 28

issue 110

23-34

Continuing our efforts in developing potent α 1 -adrenoceptor antagonists with uroselective profile, a series of derivatives of pyrrolidines was biologically evaluated in vitro for their affinity for α 1 - and α 2 -adrenoceptors. Result from binding assays allowed the identification of compounds with the highest affinity and selectivity for α 1 -adrenoceptors behaving as potent antagonists at those sites in cellular functional assays. Among tested derivatives, compound V [1-(3-(4-(3- chlorophenyl)piperazin-1-yl)propyl)pyrrolidin-2-one], displayed a 152-fold functional preference to α 1A -adrenoceptor versus α 1B subtype. Finally, the most promising compound V at the doses of 2, 5 and 10 mg/kg after i.v. administered, in contrast to tamsulosin (at a dose of 2 mg/kg, i.v.) did not significantly decrease systolic and diastolic blood pressure in normotensive anesthetized rats. This selected α 1A -adrenoceptor antagonist with stronger uroselective profile, requires further research.

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1 Medicina Internacia Revuo

1 2018

1 BELCZYK M.

1 Bednarski M.

1 Knutelska J.

1 Kotańska M.

1 LECHOCKA-NOWAK A.

1 Nowiński L.

1 Sapa J.

1 ZYGMUNT M.

1 Zaręba P.

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PHARMACOLOGICAL EVALUATION OF PYRROLIDINES AS POTENT ! 1 - ADRENERGIC RECEPTOR ANTAGONIST WITH URO-SELECTIVE PROFILE