Effects of histamine and the histamine antagonists mepyramine and cimetidine on human coronary arteries <i>in vitro</i>

Godfraind, Théophile; Miller, Robert C.

doi:10.1111/j.1476-5381.1983.tb10544.x

Cited by 26 publications

(11 citation statements)

References 15 publications

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“…In ring preparations of isolated rabbit mesenteric arteries, we have observed that histamine elicits mepyramine-sensitive contractions ; indicating an action via HI receptor activation as previously reported for other blood vessels (Godfraind and Miller, 1983; Van de Voorde and Leusen, 1984;Toda, 1986). The present study shows a competitive antagonism of histamine-mediated responses by cicletanine, comparable to observations in guinea-pig ileum (Schoeffter et al, 1987) and human coronary artery (Schoeffter and Godfraind, 1988); thus suggesting an action via H1 receptors.…”

Section: Discussionsupporting

confidence: 86%

“…It could be reasoned that the biphasic response to histamine in cicletamine-treated rings is a sum of 2 possible actions on the (-) and (+)-enantiomem of cicletanine in the racemic mixture employed. The distribution of histamine receptors on endothelial and smooth muscle cells has been reported to show both tissue as well as speciesspecificity (Godfraind and Miller, 1983; Van de Voorde et al, 1984;Abacioglu et al, 1987). 4).…”

Section: Discussionmentioning

confidence: 99%

“…The vascular actions of histamine are mediated through stimulation of 2 subclasses (HI and H2) of receptors, responsible for vasoconstriction and vasodilata-tion, respectively (Black et al, 1972 ;Durant et al, 1972; Godfraind and Miller, 1983;Toda, 1986). Antagonism of histamine action could be of therapeutic importance in view of the physiologic role of histamine in the regulation of vascular tone (Ginsburg et al, 1980(Ginsburg et al, , 1981Ebeigbe et al, 1983; Godfraind and Miller, 1983; Ebeigbe, 1986).…”

Section: Introductionmentioning

confidence: 99%

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Effects of Cicletanine on Histamine‐induced Contractions of Isolated Rabbit Mesenteric Arteries

Ebeigbe

Cabanie²,

Godfraind

1989

Fundamemntal Clinical Pharma

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The antagonism by cicletanine of contractile responses to histamine has been examined in vitro on ring preparations of rabbit mesenteric arteries. Cicletanine (10(-8)-10(-6) M) caused a parallel rightward shift of histamine concentration response curve, with a pA2 value of 7.48 (slope = 0.89 +/- 0.19, not significantly different from unity). Histamine-induced contractions were nifedipine-sensitive and associated with cicletanine-sensitive increased 45Ca uptake. Endothelium removal resulted in enhanced contractile responses to histamine, but did not significantly modify cicletanine-induced antagonism: KB (dissociation constant) values for cicletanine antagonism in the presence or absence of endothelium were: 3.7 (+/- 0.1) X 10(-8) M and 3.6 (+/- 0.3) X 10(-8) M, respectively. Cicletanine (greater than 10(-4) M) also significantly attenuated 10 mM caffeine-induced contractions in rings exposed to Ca-free 100 mM K+ depolarizing medium. The results suggest that cicletanine-induced antagonisms of histamine H1 receptor-mediated contractions of rabbit mesenteric arteries is associated with interference with calcium entry as well as at high concentrations, release from intracellular stores.

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Section: Discussionsupporting

confidence: 86%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Effects of Cicletanine on Histamine‐induced Contractions of Isolated Rabbit Mesenteric Arteries

Ebeigbe

Cabanie²,

Godfraind

1989

Fundamemntal Clinical Pharma

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“…Terminal portions (about 2 cm) of the anterior descending branch of the left coronary artery and circumflex coronary artery were removed and cleaned of all loosely adherent tissue. Rings of artery (about 2 mm wide) were suspended in 50 ml organ baths in physiological solution (composition millimolar: NaC1,112;KCI,5;NaHCO,,25;KH~POI,0.1;MgS04,0.12;CaC12,1.25;and glucose,11.5) maintained at 37" and aerated with a gas mixture of 95% 0 2 and 5% C02 under a resting tension of 2 g. The presence of endothelium in these preparations was demonstrated by their relaxant response to histamine (Godfraind & Miller 1983b;Van de Voorde & Leusen 1983). Sixteen rings were prepared from each heart.…”

Section: Methodsmentioning

confidence: 99%

The Actions of Nifedipine and Nisoldipine on the Contractile Activity of Human Coronary Arteries and Human Cardiac Tissue in Vitro

Godfraind

Eglème

Finet

et al. 1987

Pharmacology & Toxicology

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We have studied the action of nifedipine and nisoldipine on the contractile activity of human isolated coronary arteries and human isolated auricular and ventricular muscles. Nisoldipine depressed dose dependently the spontaneous rhythmic contractions displayed by the coronary artery preparations and at 1 nM abolished these contractions. Nisoldipine was twenty times more potent than nifedipine as an inhibitor of increase in tone induced by depolarization (100 mM K+). The rhythmic activity induced by serotonin (10 microM) was about five times more sensitive to nisoldipine than to nifedipine. In both auricular and ventricular preparations, isoprenaline evoked an increase in the rate of force development and in the rate of relaxation. Nifedipine was five times (ventricular muscles) and ten times (auricular muscles) more potent than nisoldipine as a negative inotropic agent. The present observations in human isolated preparations indicate that nisoldipine shows a higher vascular selectivity than nifedipine.

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“…Studies using selective histamine-receptor agonists and antagonists have demonstrated the presence of coronary vasoconstricting H, receptors and vasodilating H 2 receptors in isolated epicardial vessels. '-2 -2 *" 31 When coronary blood flow is the measured variable, in situ and in vivo data indicate that histamine-induced increases are mediated by both H, and H 2 receptor. 4 -3 -32 - 33 While this apparent disparity in findings has produced some confusion, it does suggest a basis for the separate regulation and responsiveness of epicardial conductance and distal resistance arteries.…”

Section: Discussionmentioning

confidence: 99%

Differential H1- and H2-receptor-mediated histamine responses of canine epicardial conductance and distal resistance coronary vessels.

Miller

Bové

1988

Circulation Research

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The contributions of histamine (H1 or H2) receptor-mediated responses and, therefore, the effects of histamine blocking agents are unclear with regard to regulation of proximal epicardial and distal resistance coronary arteries. This study was designed to evaluate the effects of selective H1- and H2-receptor antagonists on epicardial and resistance vessels in the closed chest dog model. Histamine, diphenhydramine (H1 blocker), and cimetidine (H2 blocker) were infused into the left anterior descending coronary artery (LAD), and responses were studied by quantitative coronary angiography and flow measurements (133Xe washout). Histamine infusion alone produced a significant dilation of the proximal LAD (13% above control) only at the highest dose (45 micrograms/min), while LAD flow was increased by 128%. In the presence of H1 blocker, histamine produced significantly greater epicardial dilation (55% above control). The flow response curve was shifted to the right in the presence of H1 blocker, but the flow attenuation was overcome by the highest histamine dose. In contrast, the H2 blocker attenuated both epicardial dilation (6% below control) and flow response (31% above control) to the highest histamine dose. Results support a differential regulation of proximal epicardial and distal resistance vessels to histamine with epicardial arteries demonstrating H1-mediated vasoconstriction and H2-mediated vasodilation and distal resistance vessels showing H1- and H2-mediated vasodilation. In addition, these findings suggest that H1 blockade may antagonize histamine-related vasoconstriction and vasospasm, while H2 blockers may permit unopposed H1-mediated vasoconstriction of epicardial arteries and also limit resistance vessel vasodilatory responsiveness in the presence of elevated tissue histamine, as may occur in atherosclerotic coronary artery disease.

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Effects of histamine and the histamine antagonists mepyramine and cimetidine on human coronary arteries in vitro

Cited by 26 publications

References 15 publications

Effects of Cicletanine on Histamine‐induced Contractions of Isolated Rabbit Mesenteric Arteries

Effects of Cicletanine on Histamine‐induced Contractions of Isolated Rabbit Mesenteric Arteries

The Actions of Nifedipine and Nisoldipine on the Contractile Activity of Human Coronary Arteries and Human Cardiac Tissue in Vitro

Differential H1- and H2-receptor-mediated histamine responses of canine epicardial conductance and distal resistance coronary vessels.

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