The effect of ketanserin, a 5-HT2-receptor antagonist, on 5-hydroxytryptamine-induced irreversible platelet aggregation in patients with cardiovascular diseases

@article{Cre1985TheEO,
  title={The effect of ketanserin, a 5-HT2-receptor antagonist, on 5-hydroxytryptamine-induced irreversible platelet aggregation in patients with cardiovascular diseases},
  author={J. De Cr{\'e}e and Jos Leempoels and B Demoen and V. Roels and Herman Verhaegen},
  journal={Agents and Actions},
  year={1985},
  volume={16},
  pages={313-317},
  url={https://api.semanticscholar.org/CorpusID:20280192}
}
Treatment with ketanserin might be of therapeutic value in atherosclerotic diseases, where platelet activation is thought to be involved and 5-HT is a potent mediator of vasospam.
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6 Citations

Serotonin-induced platelet aggregation predicts the antihypertensive response to serotonin receptor antagonists

The present data suggest that the blood pressure response to ketanserin can be predicted from the ex vivo sensitivity of platelets to serotonin, and this support a role for serotonergic mechanisms in hypertension.

Hyperreactivity of Platelets to Serotonin (5-Hydroxytryptamine) in Patients with Cardiovascular Diseases

The effects on serotonin-induced irreversible platelet aggregation of ketanserin, a specific serotonin Srreceptor antagonist effective against both vascular and platelet serotonergic receptor activation (Van Nueten et al. 1987), were studied.

Effects of ketanserin, a selective 5-HT2 serotonergic antagonist, on the secondary recruitment of human plateletsin vitro

Ketanserin reduces in vitro the release-associated human platelet aggregation induced by threshold concentrations of collagen and curtails the second wave of aggregation/release induced by critical concentrations of ADP in particular and, to a lesser extent, of 1-epinephrine.

Serotonin Metabolism and Age-Related Effects of Antihypertensive Therapy with Ketanserin

Antihypertensive therapy with ketanserin reduced platelet aggregation and serotonin metabolism in relation to the age of patients, and this may contribute to the reduction of their elevated rates of thromboembolic complications.

Ketanserin

Ketanserin appears that its antihypertensive activity is suited to the elderly provided plasma potassium concentrations are normal at the start of treatment and are maintained within the normal range, and the frequency of adverse effects being comparable with that of other antihypertensive drugs in controlled trials.

Comparison of ketanserin and enalapril in the treatment of mild-to-moderate essential hypertension

Ketanserin is as effective and well tolerated as enalapril in hypertensive patients over 50 years of age, and no changes occurred in mean blood pressure, heart rate or in biochemical variables.

29 References

Inhibition of 5-hydroxytryptamine-induced and-amplified human platelet aggregation by ketanserin (R 41 468), a selective 5-HT2-receptor antagonist

The present evidence suggests the presence of functional 5-HT2 receptors on the human platelet, different from those involved in the uptake of the monoamine, as well as the active uptake of14C-5-HT by platelets.

The Antihypertensive Effects of a Pure and Selective Serotonin-Receptor Blocking Agent (R 41 468) in Elderly Patients

Essential hypertension might be causally related to an impair ment of venous function, in which serotonin might be an important pressor factor, and R 41 468 most probably acts by decreasing the venous capacitance bed constriction.

The involvement of 5-HT2-receptor sites in the activation of cat platelets.

Effects of ketanserin and mepyramine on platelet aggregation and on the uptake of 5-hydroxytryptamine into platelets.

Influence of lysolecithin on platelet aggregation initiated by 5-hydroxytryptamine.

The results failed to confirm that irreversible platelet aggregation initiated in vitro by adenosine diphosphate, adrenaline or collagen was inhibited by lysolecithin, whilst reversible ADP-induced aggregation was unaffected and 5-HT was found on occasions to initiate biphasic aggregation resembling that induced by ADP.

Treatment of hypertension with ketanserin, a new selective 5-HT2 receptor antagonist.

The new selective 5-HT2 receptor blocking agent ketanserin was given in a dose of 10 mg intravenously to 12 patients with essential hypertension, causing dilatation of both resistance and capacitance vessels and of the renal vascular bed, suggesting that 5- HT may have a role in maintaining high blood pressure.

Vascular effects of ketanserin (R 41 468), a novel antagonist of 5-HT2 serotonergic receptors.

Plasma beta-thromboglobulin as a measure of platelet activity. Effect of risk factors and findings in ischemic heart disease and after acute myocardial infarction.

Platelet Aggregates in Ischemic Heart Disease

The occurrence of platelet aggregates in venous blood in regard to the type and location of myocardial infarction; the phase of myCardial ischemia (stable versus unstable angina); the temporal relationship between an episode of ischemIA and an increase in platelets; and the possible correlation of these to such factors as patient's age, platelet count, leukocytosis, and enzyme elevation are studied.

Platelet-mediated vascular contractions: inhibition of the serotonergic component by ketanserin.

In vitro stimulation of washed rat platelets with thrombin as well as their activation on de-endothelialized vascular preparations, produced a strong contraction of isolated rat caudal arteries that was effectively reduced by ketanserin, a selective 5-HT2 receptor antagonist.