5-Ht2-Receptor Blockade in the Treatment of Heart Failure

Demoulin, J. C.; Soumagne, D; Bertholet, M; David, Jean-Louis; Kulbertus, HenriE

doi:10.1016/s0140-6736(81)92352-7

Cited by 38 publications

(13 citation statements)

References 6 publications

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“…It favorably influenced the myocardial energy requirements as indicated by the decrease in rate-pressure product or triple product. The acute reduction in blood pressure was accompanied by a transient stimulation of the sympathetic system and by a slight transient rise in heart rate [De Cr6e et al, 1981, 1985aDemoulin et al, 1981;Fagard et al, 1984;Wenting et al, 1984;and unpublished data]. Intravenous antihypertensive treatment with ketanserin was found useful in pre-and postoperative hypertension and in hypertensive crises in preeclampsia [Montenegro et al, 1985;Van der Starre et al, 1983;Weiner, 1985;and unpublished data].…”

Section: Acute Antihypertensive and Hemodynamic Effectsmentioning

confidence: 99%

Ketanserin: A novel cardiovascular drug

Symoens

Janssens

1986

Drug Development Research

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Symoens, J. and M. Janssens: Ketanserin: A novel cardiovascular drug. Drug Dev. Res. 8:159-172, 1986. Extensive clinical investigation has shown that ketanserin is an effective first-line antihypertensive agent with particular advantages in older patients. It has a favorable hemodynamic profile and seems devoid of serious side-effects. Clinical studies in various diseases indicate a gradual improvement of the microcirculation, which is compatible with selective serotonin S2-antagonism. Ketanserin has a favorable influence on several cardiovascular risk factors. Preliminary data suggest that it has vascular protective effects in patients with atherosclerosis.

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Section: Acute Antihypertensive and Hemodynamic Effectsmentioning

confidence: 99%

Ketanserin: A novel cardiovascular drug

Symoens

Janssens

1986

Drug Development Research

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“…198 Correlation between antagonism of mescaline, and of bilateral clonic seizures of the forepaws ( 0 ) and I98 1 ; Vanhoutte, 1982: Wenting et al, 19821, Periphcral serotonin S2 antagonism also appears to be the basis of ketanserin's activity in various other vascular diseases, such as acute thrombotic episodes, heart failure, and peripheral vascular disorders [De Moulin et al, 1981;Jageneau et al, 1983;Miranda et al, 1982;for review, see Symoens, 19821. Pirenperone is a potent antagonist of LSD's discriminative stimulus properties in the rat [Colpaert et al, 19821; it differs from other purported antagonists in that it exerts no agonist effects.…”

Section: -Htp Antagonistsmentioning

confidence: 99%

Mescaline‐induced head‐twitches in the rat: An in vivo method to evaluate serotonin S₂ antagonists

Niemegeers

Colpaert

Leysen

et al. 1983

Drug Development Research

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An intravenous dose of 20.0 mg/kg of mescaline induced a reproducible head-twitch response in rats. Drugs with very different pharmacological activities were tested for potential inhibition of this response. Among these drugs were a large number of serotonin antagonists, including several members of the recently described selective Sp antagonists of which ketanserin (a potent vascular Sp antagonist) and pirenperone (a pure LSD antagonist) are two prototypes. The same compounds were further studied in six in vivo tests in rats; these tests presumably measure antagonism at sites responsive to serotonin, dopamine, norepinephrine, histamine, or acetylcholine. A large number of test compounds inhibited mescaline-induced head-twitches. Although it was often associated with it, this activity did not correlate with any of the following effects: antagonism of apomorphine, norepinephrine, compound 48/80, physostigmine, or with mydriatic activity. Antagonism of mescaline did correlate, however, with in vivo antagonism of tryptamine and 5-hydroxytryptophan, and with inhibition of 3H-spiperone binding to the rat prefrontal cortex in vitro. It is concluded that inhibition of mescaline-induced head-twitches in the rat is a valid measure of serotonin Sp antagonist activity, also for those compounds whose primary activity occurs at dopamine, norepinephrine, histamine, or acetylcholine receptors. Ketanserin, pirenperone, and several chemically related compounds are very potent mescaline antagonists.

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“…3,JT: indirect LA pressure: 29 mm Hg). Venous dilatation has been demonstrated previously (Demoulin et al, 1981;Wenting et al, 1982), and such a mechanism would explain the observed fall in the pulmonary artery diastolic pressure. Thus lower filling pressures and vascular resistances would all contribute to the marked fall in left ventricular systolic pressure and thus account for the fall in coronary blood flow that was measured.…”

Section: Discussionmentioning

confidence: 61%

“…The pharmacological profile of this drug make it very suitable for the investigation of 5-HT2 receptors in clinical conditions where the control of vascular tone is likely to be of pathological importance and therapeutic interest. Clinical studies have confirmed that ketanserin has an effect on the peripheral circulation, causing dilatation of resistance and capacitance vessels in hypertensive subjects (DeCree et al, 1981;Wenting et al, 1982) and significant falls in pre-load and afterload in heart failure patients (Demoulin et al, 1981). We have examined the effects of an intravenous dose of ketanserin in patients undergoing cardiac catheterisation for various severities of ischaemic heart disease.…”

Section: Introductionmentioning

confidence: 94%

Acute effects of ketanserin on left ventricular function, metabolism and coronary blood flow.

Walker¹,

Wilmshurst²,

Juul³

et al. 1984

Brit J Clinical Pharma

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1 An acute intravenous bolus of 10 mg ketanserin (a specific 5-HT antagonist) caused an abrupt fall in left ventricular systolic pressure of 17 + 9.2 mm Hg (P < 0.025) in ten patients undergoing cardiac catheterisation for chest pains. 2 A fall in pulmonary artery diastolic pressure of 2.1 + 0.74 mm Hg (P < 0.02) was also observed. 3 No changes in resting heart rate occurred and the response to pacing was largely unmodified by ketanserin, except for a reduction in pulmonary vascular resistancte (3.70 ± 1.27 units to 2.97 + 1.44 units, P < 0.05), at the fastest rate (136 + 3 beats/min). 4 At the highest pacing rate coronary sinus blood flow fell (83 ± 12 ml 100 g-min-to 68 + 8 ml 100 g-1 min-', P < 0.05), as did myocardial oxygen consumption (18 + 2 ml-min to 14 + 1 ml min-', P < 0.05) after the drug. 5 No changes in the parameters of left ventricular contractile function could be attributed to ketanserin, save for a modest increase in the ejection fraction (48 + 6% to 57 ± 6%, P < 0.05) in seven patients. 6 There were no alterations in myocardial metabolism of lactate, pyruvate, hydroxybutyrate, glycerol nor free fatty acids after ketanserin. 7 The findings are consistent with a peripheral site of action of this drug and its blood pressure lowering effect in the subjects suggest a non-specific hypotensive action rather than an anti-hypertensive effect.

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5-Ht2-Receptor Blockade in the Treatment of Heart Failure

Cited by 38 publications

References 6 publications

Ketanserin: A novel cardiovascular drug

Ketanserin: A novel cardiovascular drug

Mescaline‐induced head‐twitches in the rat: An in vivo method to evaluate serotonin S₂ antagonists

Acute effects of ketanserin on left ventricular function, metabolism and coronary blood flow.

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5-Ht2-Receptor Blockade in the Treatment of Heart Failure

Cited by 38 publications

References 6 publications

Ketanserin: A novel cardiovascular drug

Ketanserin: A novel cardiovascular drug

Mescaline‐induced head‐twitches in the rat: An in vivo method to evaluate serotonin S2 antagonists

Acute effects of ketanserin on left ventricular function, metabolism and coronary blood flow.

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Product

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Mescaline‐induced head‐twitches in the rat: An in vivo method to evaluate serotonin S₂ antagonists