Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0085580 (essential hypertension)
 14,686 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Monotherapy with Ketanserin, a serotonin receptor antagonist, reduces blood pressure in a sizeable number of patients with essential hypertension. The present study was designed to compare its antihypertensive potency with those of metoprolol in a double-blind treatment and further to study its long-term efficacy and safety in a one-year open trial, alone or combined to metoprolol, according to diastolic blood pressure (DBP) normalization. Twenty-four patients with mild to moderate hypertension were randomly assigned to two parallel treatment groups, one group (n = 11) received Ketanserin (40 mg/day) and the other one (n = 13) metoprolol (200 mg/day). After 3 months double-blind treatment, all patients received Ketanserin, on an open basis for one year alone or combined to metoprolol if Ketanserin failed to normalize DBP. A significant antihypertensive effect was demonstrated after 3 months double-blind treatment, for Ketanserin and metoprolol, in both standing and supine position (p less than 0.01). Heart rate showed a clear decrease by metoprolol (p less than 0.01). In the one-year follow-up, patients were divided in: I (n = 7) patients on Ketanserin (previously treated with the same drug); II (n = 4) patients on Ketanserin plus metoprolol (previously treated with Ketanserin, in whom it failed to normalize DBP); and III (n = 13) patients on Ketanserin (previously treated with metoprolol). In group I the blood pressure lowering effect of Ketanserin remained constant after one-year follow-up. In group II, although the number of patients was insufficient, a trend in the decrease of parameters was observed. In group III, supine and standing DBP diminished from 92.5 +/- 8 and 92.5 +/- 7 during treatment with metoprolol to 83.6 +/- 9 and 79.8 +/- 8 mmHg respectively at 12 months, after treatment with Ketanserin (p less than 0.05); accordingly, the cumulative percentage of normalized DBP increased from 4/13 after metoprolol to 12/13 at the end of the trial. Ketanserin side effects were minimal. Taking into account the wide variety of contraindications or side effects with beta-blockers and diuretics, Ketanserin appears as a new and important alternative in the treatment of mild and moderate essential hypertension.
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PMID:Ketanserin in the treatment of essential hypertension. A double-blind study against metoprolol and a further long-term open treatment. 354 22

Ketanserin, a serotonin receptor antagonist (S2), lowered blood pressure in patients with essential hypertension; at three months 72% (13/18) had a successful reduction in pressure. No marked orthostatic changes were noted. Older patients responded better when standing. Compared with metoprolol, ketanserin provided no significant difference in response at three months. With ketanserin, the heart rate was reduced only in the supine position, whereas it was reduced in the supine and standing positions with metoprolol. Response to ketanserin could not be predicted from baseline renin, aldosterone, or cortisol levels in blood, nor were there any changes in these factors or in plasma hydroxyindole levels with therapy. Ketanserin was generally well tolerated. Cholesterol values were significantly reduced with ketanserin, and there were no adverse hematologic or biochemical changes. Ketanserin should have a significant role in managing hypertension.
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PMID:Comparison of ketanserin and metoprolol in the treatment of essential hypertension. 354 16

Ketanserin is a new, specific serotonin receptor blocking agent, which causes vasodilatation, presumably by an action on the vascular wall. The antihypertensive response to ketanserin 40 mg twice daily as monotherapy was assessed in 8 patients with essential hypertension. The investigation was an 8 week, double-blind, cross over study, which also included measurements during isometric (handgrip) and dynamic exercise (bicycle ergometry), as well as determination of plasma catecholamines and ketanserin. Ketanserin caused a reduction of supine and standing systolic and diastolic blood pressure (BP) during rest and a slight bradycardia. Although there was attenuation of the pressor response to handgrip, treatment with ketanserin did not really affect the changes in BP or heart rate during exercise, i.e. the base-line differences remained the same. There was no significant correlation between the effect on BP and the plasma level of ketanserin. The changes in BP produced by ketanserin showed little correlation with the initial levels of plasma catecholamines or with alterations in those levels. Although the results did not indicate direct interference by ketanserin with sympathetic tone, the lack of reflexogenic tachycardia, as well as the lack of increase in plasma noradrenaline during hand grip, indicates at least some modulation of autonomic function. It is concluded that ketanserin lowers BP in essential hypertension without interference with cardiovascular reflexes during standing or exercise, and that the compound may offer an alternative approach in the treatment of hypertension.
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PMID:Ketanserin in essential hypertension: effects during rest and exercise. 662 17

The 5-HT1A receptor is a pharmacologically well characterized serotonin receptor subtype and it has long been investigated because of its involvement in several physiopathological mechanisms and treatment of neurological diseases like ansia and depression. Serotonin (5-HT) also shows many non-neural functions such as essential hypertension, embryogenesis, follicle maturation and behavior. Moreover, it exerts a growth factor function on different types of non-tumoral cells, and it was also found to be related to oncogenes. In fact, growth-stimulatory activity of serotonin in different human tumor cells has been reported. Recently, new chemical molecules binding the 5-HT1A receptor have been described as novel therapeutic entities useful in neuroprotection, cognitive impairment, Parkinson's Disease, pain treatment, malignant carcinoid syndrome and cancer. It was widely demonstrated that 5-HT1A receptor is involved in the carcinogenesis and consequently in many human tumor types, such as prostate, bladder, small cell lung, colonrectal and cholangiocarcinoma. Furthermore, depending on the tumor type, 5-HT1A receptor antagonists were shown to be capable of blocking the 5HT-induced increase in tumor growth. In this review, we have focused our attention on each tumor type where the 5-HT1A receptor is involved, investigating the role of this molecular target and the different classes of compounds that have shown the capability to modulate it. The analyzed aspects could represent a hint for the medical chemists to develop novel molecules as selective 5-HT1A agents are useful in further elucidating the role of this therapeutic target.
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PMID:The Role of 5-HT1A Receptor in Cancer as a New Opportunity in Medicinal Chemistry. 2942 2