- Tytuł:
- PHARMACOLOGICAL EVALUATION OF PYRROLIDINES AS POTENT ! 1 - ADRENERGIC RECEPTOR ANTAGONIST WITH URO-SELECTIVE PROFILE
- Autorzy:
-
Sapa, Jacek
Bednarski, Marek
Nowiński, Leszek
Kotańska, Magdalena
Knutelska, Joanna
Zaręba, Paulina
LECHOCKA-NOWAK, Anna
BELCZYK, Małgorzata
ZYGMUNT, Małgorzata - Powiązania:
- https://bibliotekanauki.pl/articles/956844.pdf
- Data publikacji:
- 2018
- Wydawca:
- Zakład Opieki Zdrowotnej Ośrodek Umea Shinoda-Kuracejo
- Tematy:
- α1A/B receptor selectivity
- Opis:
- 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.
- Źródło:
-
Medicina Internacia Revuo; 2018, 28, 110; 23-34
0465-5435 - Pojawia się w:
- Medicina Internacia Revuo
- Dostawca treści:
- Biblioteka Nauki
Artykuł