fk-838 and 1-3-dipropyl-8-cyclopentylxanthine

fk-838 has been researched along with 1-3-dipropyl-8-cyclopentylxanthine* in 2 studies

Other Studies

2 other study(ies) available for fk-838 and 1-3-dipropyl-8-cyclopentylxanthine

Article	Year
Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. Bioorganic & medicinal chemistry letters, 1999, Jul-19, Volume: 9, Issue:14 Novel 3-(2-cycloalkyl and cycloalkenyl-3-oxo-2,3-dihydropyridazin-6-yl)-2-phenylpyrazo lo [1,5-a]-pyridines were synthesized and evaluated for their adenosine A1 receptor binding activities. In this series, FR166124 (3) was found to be the most potent and selective adenosine A1 receptor antagonist, and the double bond of the cyclohexenyl acetic acid group was essential for selectivity of A1 receptor binding. Furthermore, the solubility in water of the sodium salt of FR 166124 was high. Topics: Antihypertensive Agents; Inhibitory Concentration 50; Molecular Structure; Piperidines; Purinergic P1 Receptor Antagonists; Pyrazoles; Pyridines; Receptors, Purinergic P1; Solubility; Structure-Activity Relationship; Water; Xanthines	1999
[Effect of adenosine on isolated afferent arterioles]. Nihon Jinzo Gakkai shi, 1999, Volume: 41, Issue:7 We investigated the direct effect of adenosine on afferent arterioles (Af-Arts) and the receptor subtype that mediates the constrictor or dilator action of adenosine. Af-Arts were isolated from the superficial cortex of rabbit kidney and perfused in vitro. Adenosine added to either the lumen or bath constricted the Af-Arts in a dose-dependent manner. This constriction was blocked by the A1 receptor antagonist, 6-oxo-3-(2-phenylpyrazole(1,5-a)pyridin-3-yl)-1 (6H)-pyridazinebutyric acid (FK838) or 8-cyclopentyl-1, 3-dipropylxanthine(DPCPX). We also examined the effect of adenosine on preconstricted Af-Arts with norepinephrine. Adenosine added to either the lumen or bath further constricted the preconstricted Af-Arts. In the presence of FK838, adenosine added to either the lumen or bath dilated the preconstricted Af-Arts, but in a different dose-dependent manner. Adenosine-induced dilation was inhibited by the A2 receptor antagonist, 3, 7-dimetyl-1-propargylxanthine(DMPX). These data indicate that adenosine constricts Af-Arts via A1 receptors and that adenosine dilates preconstricted Af-Arts via A2 receptors when A1 receptors are blocked. Topics: Adenosine; Animals; Arterioles; Dose-Response Relationship, Drug; In Vitro Techniques; Kidney; Male; Purinergic P1 Receptor Antagonists; Pyrazoles; Pyridines; Rabbits; Theobromine; Vasoconstriction; Vasodilation; Vasodilator Agents; Xanthines	1999

Article

Year

Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.

Bioorganic & medicinal chemistry letters, 1999, Jul-19, Volume: 9, Issue:14

Novel 3-(2-cycloalkyl and cycloalkenyl-3-oxo-2,3-dihydropyridazin-6-yl)-2-phenylpyrazo lo [1,5-a]-pyridines were synthesized and evaluated for their adenosine A1 receptor binding activities. In this series, FR166124 (3) was found to be the most potent and selective adenosine A1 receptor antagonist, and the double bond of the cyclohexenyl acetic acid group was essential for selectivity of A1 receptor binding. Furthermore, the solubility in water of the sodium salt of FR 166124 was high.

Topics: Antihypertensive Agents; Inhibitory Concentration 50; Molecular Structure; Piperidines; Purinergic P1 Receptor Antagonists; Pyrazoles; Pyridines; Receptors, Purinergic P1; Solubility; Structure-Activity Relationship; Water; Xanthines

1999

[Effect of adenosine on isolated afferent arterioles].

Nihon Jinzo Gakkai shi, 1999, Volume: 41, Issue:7

We investigated the direct effect of adenosine on afferent arterioles (Af-Arts) and the receptor subtype that mediates the constrictor or dilator action of adenosine. Af-Arts were isolated from the superficial cortex of rabbit kidney and perfused in vitro. Adenosine added to either the lumen or bath constricted the Af-Arts in a dose-dependent manner. This constriction was blocked by the A1 receptor antagonist, 6-oxo-3-(2-phenylpyrazole(1,5-a)pyridin-3-yl)-1 (6H)-pyridazinebutyric acid (FK838) or 8-cyclopentyl-1, 3-dipropylxanthine(DPCPX). We also examined the effect of adenosine on preconstricted Af-Arts with norepinephrine. Adenosine added to either the lumen or bath further constricted the preconstricted Af-Arts. In the presence of FK838, adenosine added to either the lumen or bath dilated the preconstricted Af-Arts, but in a different dose-dependent manner. Adenosine-induced dilation was inhibited by the A2 receptor antagonist, 3, 7-dimetyl-1-propargylxanthine(DMPX). These data indicate that adenosine constricts Af-Arts via A1 receptors and that adenosine dilates preconstricted Af-Arts via A2 receptors when A1 receptors are blocked.

Topics: Adenosine; Animals; Arterioles; Dose-Response Relationship, Drug; In Vitro Techniques; Kidney; Male; Purinergic P1 Receptor Antagonists; Pyrazoles; Pyridines; Rabbits; Theobromine; Vasoconstriction; Vasodilation; Vasodilator Agents; Xanthines

1999