N-Methyl-2-pyridone-5-carboxamide is 1-methylnicotinamide metabolite of low cyclooxygenase-dependent vasodilating activity

The effects of prostaglandins E1, E2, and F2alpha (PGE1, PGE2, and PGE2alpha, respectively) on uterine blood flow were investigated in chronically catheterized, nonpregnant sheep equipped with electromagnetic flow probes. PGE1 was found to be a potent dilator of the uterine vascular bed and, at initial arterial concentratios of 1.5 micron (500 ng/ml), produced peak uterine blood flows similar to those achieved by a pulsed dose of 1 microgram 17beta-estradiol; PGE2 had less active vasodilating activity. Conversely, uterine intra-arterial PGF2alpha infusions, which produced initial concentrations of 0.1 micron (50 ng/ml), promptly reduced peak estrogen-stimulated uterine blood flow by 60%. All prostaglandin infusions stimulated increases in uterine contractile frequency and base-line tone. The findings demonstrate the sensitivity of the nonpregnant sheep uterine vasculature to prostaglandins.

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PDGF-BB decreases systolic blood pressure through an increase in macrovascular compliance in rats

AJP Heart and Circulatory Physiology ◽

10.1152/ajpheart.1997.273.4.h1719 ◽

1997 ◽

Vol 273 (4) ◽

pp. H1719-H1726 ◽

Cited By ~ 3

Author(s):

Masahiro Ikeda ◽

Chizuru Morita ◽

Makoto Mizuno ◽

Toshio Sada ◽

Hiroyuki Koike ◽

...

Keyword(s):

Blood Pressure ◽

Diastolic Pressure ◽

Contractile Activity ◽

Isolated Heart ◽

Systolic Pressure ◽

Hypotensive Effect ◽

Platelet Derived Growth Factor ◽

High Concentration ◽

Vasodilating Activity

The cardiovascular roles of platelet-derived growth factor (PDGF) were examined in anesthetized rats by monitoring blood pressure and in isolated blood vessels and heart preparations. Intravenous injection of PDGF-BB lowered blood pressure. The decrease in systolic pressure was greater than that in diastolic pressure, so the pulse pressure decreased. PDGF-AA and -AB, other isoforms of PDGF, did not have any effect on blood pressure. Pretreatment of rats with Nω-nitro-l-arginine methyl ester (l-NAME), an inhibitor of nitric oxide (NO) synthase, shortened duration of the hypotensive effect of PDGF-BB. The administration ofl-arginine withl-NAME partially prevented the effect of l-NAME. PDGF-BB relaxed aortic rings precontracted with phenylephrine with a 50% effective concentration of 3 ng/ml. In contrast, in isolated mesenteric vascular preparations, the vasodilating activity of PDGF-BB was observed only at a high concentration (>12.5 ng/ml). In isolated heart preparations, PDGF-BB had no effect on the beat rate or contractile activity. These results suggest a new role of PDGF-BB that may contribute to the regulation in circulation through the increase in macrovascular compliance mediated by NO.

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ChemInform Abstract: 1,2-Diazetine 1,2-Dioxide Derivatives: A New Class of Nitrogen Oxide Generators with Vasodilating Activity

ChemInform ◽

10.1002/chin.199437093 ◽

2010 ◽

Vol 25 (37) ◽

pp. no-no

Author(s):

G. YA. SHVARTS ◽

N. B. GRIGOR'EV ◽

I. S. SEVERINA ◽

I. K. RYAPOSOVA ◽

A. S. LAPITSKAYA ◽

...

Keyword(s):

Nitrogen Oxide ◽

New Class ◽

Vasodilating Activity

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Antianginal efficacy of carvedilol, a beta-blocking drug with vasodilating activity

The American Journal of Cardiology ◽

10.1016/s0002-9149(86)80010-8 ◽

1986 ◽

Vol 58 (10) ◽

pp. 916-921 ◽

Cited By ~ 17

Author(s):

Erwin A. Rodrigues ◽

Avijit Lahiri ◽

Liam O. Hughes ◽

Ravinder S. Kohli ◽

John R. Whittington ◽

...

Keyword(s):

Blocking Drug ◽

Beta Blocking ◽

Vasodilating Activity ◽

Antianginal Efficacy

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Structure of amauromine, a new alkaloid with vasodilating activity produced by sp.

Tetrahedron Letters ◽

10.1016/s0040-4039(01)91230-4 ◽

1984 ◽

Vol 25 (41) ◽

pp. 4673-4676 ◽

Cited By ~ 20

Author(s):

Shigehiro Takase ◽

Yoshio Kawai ◽

Itsuo Uchida ◽

Hirokazu Tanaka ◽

Hatsuo Aoki

Keyword(s):

Vasodilating Activity

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Effect of Propofol on Norepinephrine-induced Increases in [Ca2+](i) and Force in Smooth Muscle of the Rabbit Mesenteric Resistance Artery

Anesthesiology ◽

10.1097/00000542-199806000-00021 ◽

1998 ◽

Vol 88 (6) ◽

pp. 1566-1578 ◽

Cited By ~ 25

Author(s):

Nami Imura ◽

Yoshihisa Shiraishi ◽

Hirotada Katsuya ◽

Takeo Itoh

Keyword(s):

Smooth Muscle ◽

Isometric Force ◽

Resistance Artery ◽

Resistance Arteries ◽

High K ◽

Small Resistance ◽

Vasodilating Activity ◽

Mesenteric Resistance Artery

Background Propofol (2,6-diisopropylphenol) possesses vasodilating activity in vivo and in vitro. The propofol-induced relaxation of agonist-induced contractions in small resistance arteries has not been clarified. Methods The effect of propofol was examined on the contractions induced by norepinephrine and high K+ in endothelium-denuded rabbit mesenteric resistance artery in vitro. The effects of propofol on the [Ca2+]i mobilization induced by norepinephrine and high K+ were studied by simultaneous measurement of [Ca2+]i using Fura 2 and isometric force in ryanodine-treated strips. Results Propofol attenuated the contractions induced by high K+ and norepinephrine, the effect being greater on the high K+-induced contraction than on the norepinephrine-induced contraction. In Ca2+-free solution, norepinephrine produced a transient contraction resulting from the release of Ca2+ from storage sites that propofol attenuated. In ryanodine-treated strips, propofol increased the resting [Ca2+]i but attenuated the increases in [Ca2+]i and force induced by both high K+ and norepinephrine. In the presence of nicardipine, propofol had no inhibitory action on the residual norepinephrine-induced [Ca2+]i increase, whereas it still modestly increased resting [Ca2+]i, as in the absence of nicardipine. Conclusions In smooth muscle of the rabbit mesenteric resistance artery, propofol attenuates norepinephrine-induced contractions due to an inhibition both of Ca2+ release and of Ca2+ influx through L-type Ca2+ channels. Propofol also increased resting [Ca2+]i, possibly as a result of an inhibition of [Ca2+]i removal mechanisms. These results may explain in part the variety of actions seen with propofol in various types of vascular smooth muscle.

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