Effect of Labetalol on Human Platelet Function

Anfossi, Giovanni; Trovati, Mariella; Lanzio, M; Mularoni, E.; Massucco, Paola; Emanuelli, G

doi:10.1111/j.1440-1681.1988.tb01099.x

Cited by 11 publications

(3 citation statements)

References 29 publications

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“…Other -adrenoceptor antagonists (prazosin, doxazosin, urapidil, labetalol) exert slight inhibitory effects on platelet responses to catecholamine at concentrations 100-fold greater than phentolamine [351][352][353].…”

Section: Pharmacological Effects On Platelet Response To Catecholaminesmentioning

confidence: 99%

Role of catecholamines in platelet function: pathophysiological and clinical significance

Anfossi

Trovati

1996

Eur J Clin Investigation

167

107

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Platelets are involved in the pathogenesis of vascular damage in both atherosclerosis and arterial hypertension. Their reactivity in vivo is influenced by different factors, including sympathoadrenal activation, plasma levels of atherogenic lipoproteins and haemorrheological changes. In the present review, we examine the modulation of platelet function by the sympathoadrenal system and concentrate on the role of circulating catecholamines in the control of platelet responses. Human platelets exhibit both adrenergic and dopaminergic receptors that are influenced by different catecholamines. alpha(2)-Adrenoceptors of alpha(2A) subtype prevail on platelet membrane; through their stimulation, catecholamines potentiate the effects of other agonists and, at higher concentrations, initiate platelet responses, including aggregation, secretion and arachidonate pathway activation. Physiological and pathological conditions causing sympathoadrenal activation in vivo, i.e. physical activity, mental stress, insulin-induced hypoglycaemia, acute coronary ischaemia and heart failure, modify the circulating platelet populations and modulate platelet reactivity through an increase in circulating catecholamines. A sympathoadrenal hyperactivation modifies the function of circulating platelets through direct catecholamine effects, catecholamine-induced changes of haemodynamic factors and lipid pattern and inhibition of the vascular eicosanoid synthesis. The catecholamine effects on platelet function can be involved in the interplay among stress, adrenomedullary system activation and cardiovascular diseases.

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Section: Pharmacological Effects On Platelet Response To Catecholaminesmentioning

confidence: 99%

Role of catecholamines in platelet function: pathophysiological and clinical significance

Anfossi

Trovati

1996

Eur J Clin Investigation

167

107

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“…We performed prospective validation on 22 predicted compounds that have not been used as anticoagulants, and found that their coagulation activity is significantly lower than the negative controls. Among the 22 compounds, several have been reported to affect coagulation in previous research, such as labetalol 43,44 and alprenolol. 45,46 Four newly predicted compounds with lowest coagulation activity share a mutual target protein, ADRB2.…”

Section: Discussionmentioning

confidence: 99%

Tissue‐Specific Analysis of Pharmacological Pathways

Hao

Quinnies

Realubit

et al. 2018

CPT Pharmacom & Syst Pharma

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Understanding the downstream consequences of pharmacologically targeted proteins is essential to drug design. Current approaches investigate molecular effects under tissue‐naïve assumptions. Many target proteins, however, have tissue‐specific expression. A systematic study connecting drugs to target pathways in in vivo human tissues is needed. We introduced a data‐driven method that integrates drug‐target relationships with gene expression, protein‐protein interaction, and pathway annotation data. We applied our method to four independent genomewide expression datasets and built 467,396 connections between 1,034 drugs and 954 pathways in 259 human tissues or cell lines. We validated our results using data from L1000 and Pharmacogenomics Knowledgebase (PharmGKB), and observed high precision and recall. We predicted and tested anticoagulant effects of 22 compounds experimentally that were previously unknown, and used clinical data to validate these effects retrospectively. Our systematic study provides a better understanding of the cellular response to drugs and can be applied to many research topics in systems pharmacology.

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“…PRP samples (500 pL) were stirred at 37OC for 3 min in presence of buffer solution or different concentrations of verapamil or diltiazem, both without addition of the aggregating agent and following aggregation induced by 4 X 10-6 mol/ L AVP and carried out for 3 min. Samples were processed as previously described (Anfossi et al 1988). T X BZ generation was determined by radio-immunoassay (New England Nuclear, Boston, USA) and expressed as pg/ 106 platelets.…”

Section: Platelet Aggregation Studiesmentioning

confidence: 99%

Calcium‐channel Blocking Agents Verapamil and Diltiazem Are Inhibitors of Vasopressin‐induced Human Platelet Activation

Anfossi

Mularoni

Massucco

et al. 1991

Clin Exp Pharma Physio

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1. This study investigated the influences of calcium-channel blocking agents verapamil and diltiazem on platelet responses induced by arginine vasopressin (AVP) and lysine vasopressin (LVP). 2. The substances inhibited platelet aggregation induced by both low and high AVP concentrations, LVP and adrenaline plus AVP. IC50 values of each drug are lower than those determined for ADP- and collagen-elicited aggregation. Verapamil and diltiazem also decreased AVP-induced thromboxane B2 synthesis. 3. Other series of experiments showed that the addition of ethyleneglycol-bis-(beta-amino-ethyl ether) N, N'-tetra-acetic acid to platelet-rich plasma samples also prevented the platelet response to vasopressin polypeptides. 4. Our data provide evidence that the effects of verapamil and diltiazem on vasopressin-induced platelet responses may be directly related to inhibition of extracellular calcium entry.

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Effect of Labetalol on Human Platelet Function

Cited by 11 publications

References 29 publications

Role of catecholamines in platelet function: pathophysiological and clinical significance

Role of catecholamines in platelet function: pathophysiological and clinical significance

Tissue‐Specific Analysis of Pharmacological Pathways

Calcium‐channel Blocking Agents Verapamil and Diltiazem Are Inhibitors of Vasopressin‐induced Human Platelet Activation

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