Targeting Serotonin 2A and Adrenergic α1 Receptors for Ocular Antihypertensive Agents: Discovery of 3,4-Dihydropyrazino[1,2-b ]indazol-1(2H )-one Derivatives

ChemMedChem ◽  
2018 ◽  
Vol 13 (15) ◽  
pp. 1597-1607 ◽  
Author(s):  
Guido Furlotti ◽  
Maria Alessandra Alisi ◽  
Nicola Cazzolla ◽  
Francesca Ceccacci ◽  
Beatrice Garrone ◽  
...  
Keyword(s):  
Antihypertensive Agents ◽  
Α1 Receptors ◽  
Serotonin 2A

1077: Facilitation of Proceptivity/Sexual Motivation in Female Rats by a Serotonin 2A/2C (5-HT2A/2C) Receptors Agonist

2005 ◽  
Vol 173 (4S) ◽  
pp. 292-292
Author(s):  
Anne-Sophie Rössler ◽  
Jacques Bernabé ◽  
Laurent Alexandre ◽  
François Giuliano
Keyword(s):  
Sexual Motivation ◽  
Female Rats ◽  
Serotonin 2A

Long-Term Efficacy and Tolerability of a Fixed-Dose Combination of Antihypertensive Agents

2011 ◽  
pp. 1 ◽  
Author(s):  
Yiqun Wu ◽  
Yonghua Hu ◽  
Xun Tang ◽  
Liu He ◽  
Tao Ren ◽  
...  
Keyword(s):  
Antihypertensive Agents ◽  
Fixed Dose Combination ◽  
Fixed Dose ◽  
Term Efficacy ◽  
Dose Combination

Aortic Stenosis, Aortic Regurgitation and Arterial Hypertension

2019 ◽  
Vol 17 (2) ◽  
pp. 180-190 ◽  
Author(s):  
V. Katsi ◽  
G. Georgiopoulos ◽  
D. Oikonomou ◽  
C. Aggeli ◽  
C. Grassos ◽  
...  
Keyword(s):  
Aortic Valve ◽  
Aortic Stenosis ◽  
Aortic Regurgitation ◽  
Antihypertensive Agents ◽  
Renin Angiotensin System ◽  
Aortic Disease ◽  
Review Of The Literature ◽  
Angiotensin System ◽  
The Impact ◽  
Worse Prognosis

Background: Hypertension (HT) is an important risk factor for cardiovascular disease and might precipitate pathology of the aortic valve. </P><P> Objective: To investigate the association of HT with aortic dysfunction (including both aortic regurgitation and stenosis) and the impact of antihypertensive treatment on the natural course of underlying aortic disease. </P><P> Methods: We performed a systematic review of the literature for all relevant articles assessing the correlation between HT and phenotype of aortic disease. </P><P> Results: Co-existence of HT with aortic stenosis and aortic regurgitation is highly prevalent in hypertensive patients and predicts a worse prognosis. Certain antihypertensive agents may improve haemodynamic parameters (aortic jet velocity, aortic regurgitation volume) and remodeling of the left ventricle, but there is no strong evidence of benefit regarding clinical outcomes. Renin-angiotensin system inhibitors, among other vasodilators, are well-tolerated in aortic stenosis. </P><P> Conclusion: Several lines of evidence support a detrimental association between HT and aortic valve disease. Therefore, HT should be promptly treated in aortic valvulopathy. Despite conventional wisdom, specific vasodilators can be used with caution in aortic stenosis.

Arterial Stiffness, Cognitive Dysfunction and Adherence to Antihypertensive Agents. Is there a Link to Hypertensive Patients?

2020 ◽  
Vol 18 (4) ◽  
pp. 410-417 ◽  
Author(s):  
Rigas G. Kalaitzidis ◽  
Thalia Panagiotopoulou ◽  
Dimitrios Stagikas ◽  
Kosmas Pappas ◽  
Olga Balafa ◽  
...  
Keyword(s):  
Cognitive Function ◽  
Arterial Stiffness ◽  
Cognitive Dysfunction ◽  
Antihypertensive Drugs ◽  
Patient Adherence ◽  
Antihypertensive Agents ◽  
Treatment Compliance ◽  
Poor Adherence ◽  
Large Artery ◽  
Adherence To Medication

:The incidence of hypertension (HTN) and its cardiovascular (CV) complications are increasing throughout the world. Blood pressure (BP) control remains unsatisfactory worldwide. Medical inertia and poor adherence to treatment are among the factors that can partially explain, why BP control rate remains low. The introduction of a method for measuring the degree of adherence to a given medication is now a prerequisite. Complex treatment regimes, inadequate tolerance and frequent replacements of pharmaceutical formulations are the most common causes of poor adherence. In contrast, the use of stable combinations of antihypertensive drugs leads to improved patient adherence.:We aim to review the relationships between arterial stiffness, cognitive function and adherence to medication in patients with HTN.:Large artery stiffening can lead to HTN. In turn, arterial stiffness induced by HTN is associated with an increased CV and stroke risk. In addition, HTN can induce disorders of brain microcirculation resulting in cognitive dysfunction. Interestingly, memory cognitive dysfunction leads to a reduced adherence to drug treatment. Compliance with antihypertensive treatment improves BP control and arterial stiffness indices. Early treatment of arterial stiffness is strongly recommended for enhanced cognitive function and increased adherence.

Structure prediction of SPAK C-terminal domain and analysis of its binding to RFXV/I motifs by homology modelling, docking, and molecular dynamics simulation studies

2020 ◽  
Vol 16 ◽  
Author(s):  
Mubarak A. Alamri ◽  
Ahmed D. Alafnan ◽  
Obaid Afzal ◽  
Alhumaidi B. Alabbas ◽  
Safar M. Alqahtani
Keyword(s):  
Molecular Dynamic ◽  
Dynamic Stability ◽  
Md Simulation ◽  
Homology Modelling ◽  
Antihypertensive Agents ◽  
Structure And Function ◽  
Dynamics Simulation ◽  
Dimensional Structure ◽  
Terminal Domain ◽  
And Function

Background: The STE20/SPS1-related proline/alanine-rich kinase (SPAK) is a component of WNKSPAK/OSR1 signaling pathway that plays an essential role in blood pressure regulation. The function of SPAK is mediated by its highly conserved C-terminal domain (CTD) that interacts with RFXV/I motifs of upstream activators, WNK kinases, and downstream substrate, cation-chloride cotransporters. Objective: To determine and validate the three-dimensional structure of the CTD of SPAK and to study and analyze its interaction with the RFXV/I motifs. Methods: A homology model of SPAK CTD was generated and validated through multiple approaches. The model was based on utilizing the OSR1 protein kinase as a template. This model was subjected to 100 ns molecular dynamic (MD) simulation to evaluate its dynamic stability. The final equilibrated model was used to dock the RFQV-peptide derived from WNK4 into the primary pocket that was determined based on the homology sequence between human SPAK and OSR1 CTDs. The mechanism of interaction, conformational rearrangement and dynamic stability of the binding of RFQV-peptide to SPAK CTD were characterized by molecular docking and molecular dynamic simulation. Results: The MD simulation suggested that the binding of RFQV induces a large conformational change due to the distribution of salt bridge within the loop regions. These results may help in understanding the relation between the structure and function of SPAK CTD and to support drug design of potential SPAK kinase inhibitors as antihypertensive agents. Conclusion: This study provides deep insight into SPAK CTD structure and function relationship.

Antihypertensive agents for children with chronic kidney disease

2015 ◽  
Author(s):  
Arvind Bagga ◽  
Aditi Sinha ◽  
Ravindra M Pandey ◽  
Franz Schaefer
Keyword(s):  
Chronic Kidney Disease ◽  
Kidney Disease ◽  
Antihypertensive Agents

Effects of Antihypertensive Agents on Local Arterial Distensibility and Compliance

Hypertension ◽  
1995 ◽  
Vol 26 (3) ◽  
pp. 531-534 ◽  
Author(s):  
Luc M. Van Bortel ◽  
Mirian J. Kool ◽  
Harry A. Struijker Boudier
Keyword(s):  
Antihypertensive Agents ◽  
Arterial Distensibility
Sign in / Sign up

Export Citation Format

Share Document