(Hetero)Aryloxyaminopropanols with N-Phenylpiperazine Structural Fragment – Review of Cardiovascular Activity

2020 ◽  
Vol 20 (17) ◽  
pp. 1719-1731
Author(s):  
Pavlina Marvanova ◽  
Tereza Padrtova ◽  
Petr Mokry

Aryloxyphenylpiperazinylpropanols are a group of compounds exhibiting a wide range of biological activities, affecting the central nervous system and many cardiovascular mechanisms among them. As cardiovascular agents, aryloxyphenylpiperazinylpropanols work as antihypertensives, antiarrhythmics, cardiotonics or antiaggregants. The mechanism of action is almost always an α1-adrenolytic or combined α1- and β-adrenolytic effect, but sometimes other mechanisms (e.g., Ca2+ antagonism or phosphodiesterase inhibition) antagonism or phosphodiesterase inhibition) can positively participate. In some cases, compounds with a small modification of the connecting chain also exhibit the desired cardiovascular effects. Several studies dealt with chirality of aryloxyphenylpiperazinylpropanols and determined the differences between the particular activities of racemic and enantiomeric compounds.

2001 ◽  
Vol 82 (10) ◽  
pp. 2319-2326 ◽  
Author(s):  
J. D. Foster ◽  
D. W. Parnham ◽  
N. Hunter ◽  
M. Bruce

This study has examined the distribution of PrPSc in sheep by immunocytochemistry of tissues recovered from terminally affected animals following their experimental infection by the oral route with BSE. Despite a wide range of incubation period lengths, affected sheep showed a similar distribution of high levels of PrPSc throughout the central nervous system. PrPSc was also found in the lymphoid system, including parts of the digestive tract, and some components of the peripheral nervous system. These abundant PrPSc deposits in sheep in regions outside the central nervous system are in direct contrast with cattle infected with BSE, which show barely detectable levels of PrPSc in peripheral tissues. A number of genetically susceptible, challenged animals appear to have survived.


1964 ◽  
Vol 42 (1) ◽  
pp. 41-51 ◽  
Author(s):  
T. E. Emerson Jr. ◽  
C. M. Brake ◽  
L. B. Hinshaw

Little is known of the cardiovascular effects of endrin insecticide. Experiments to investigate these phenomena were carried out on dogs with a variety of preparations. Results show that acute administration of endrin produces bradycardia, hypertension, copious salivation, hyperexcitability, tonic–cionic convulsions, increased body temperature, leukocytosis, hemoconcentration, and decreased blood pH. Cerebral venous pressure and cerebrospinal fluid pressure elevations are also prominent features of endrin poisoning. Although most of these effects appear to be caused by endrin acting directly on the central nervous system some may result secondarily from altered cerebral hemodynamics.


Materials ◽  
2019 ◽  
Vol 12 (3) ◽  
pp. 465 ◽  
Author(s):  
Shoeb Ansari ◽  
Eleonora Ficiarà ◽  
Federico Ruffinatti ◽  
Ilaria Stura ◽  
Monica Argenziano ◽  
...  

Magnetic Nanoparticles (MNPs) are of great interest in biomedicine, due to their wide range of applications. During recent years, one of the most challenging goals is the development of new strategies to finely tune the unique properties of MNPs, in order to improve their effectiveness in the biomedical field. This review provides an up-to-date overview of the methods of synthesis and functionalization of MNPs focusing on Iron Oxide Nanoparticles (IONPs). Firstly, synthesis strategies for fabricating IONPs of different composition, sizes, shapes, and structures are outlined. We describe the close link between physicochemical properties and magnetic characterization, essential to developing innovative and powerful magnetic-driven nanocarriers. In conclusion, we provide a complete background of IONPs functionalization, safety, and applications for the treatment of Central Nervous System disorders.


2016 ◽  
Vol 29 (1) ◽  
pp. 14-20 ◽  
Author(s):  
Magdalena Polakowska ◽  
Jolanta Orzelska-Gorka ◽  
Sylwia Talarek

AbstractNitric oxide (NO) is a relatively novel messenger that plays a significant role in a wide range of physiological processes. Currently, it is known that, both, lack and excess of NO can cause diseases, thus a lot of substances have been discovered and utilized which can change the concentration of this molecule within the organism. The aim of the present work is to provide an overview of currently used agents modulating the L-arginine:NO:cGMP pathway, as well as to summarize current understanding of their pharmacological profiles. Nowadays, most of these agents are employed particularly in the treatment of cardiovascular diseases. Further studies can hold promise for enhancing the therapeutic equipment for a variety of other impairments, such as osteoporosis, and also in treatments of the central nervous system.


2008 ◽  
Vol 6 (1) ◽  
pp. 47-53 ◽  
Author(s):  
Agata Siwek ◽  
Monika Wujec ◽  
Maria Dobosz ◽  
Ewa Jagiełło-Wójtowicz ◽  
Anna Chodkowska ◽  
...  

AbstractBy the reaction of 2-methyl-furan-3-carboxylic acid hydrazide with isothiocyanates, 1-[(2-methyl-furan-3-yl)carbonyl]-4-substituted thiosemicarbazides 1 were obtained. Further cyclization with 2% NaOH led to the formation of 3-(2-methyl-furan-3-yl)-4-substituted-Δ2-1,2,4-triazoline-5-thiones 2. The pharmacological effects of 2 on the central nervous system in mice were investigated. Strong antinociceptive properties of the investigated derivatives were observed in a wide range of doses.


2020 ◽  
Vol 19 (1) ◽  
pp. 3-23
Author(s):  
Jianan Lu ◽  
Yujie Luo ◽  
Shuhao Mei ◽  
Yuanjian Fang ◽  
Jianmin Zhang ◽  
...  

: Melatonin is a hormone produced in and secreted by the pineal gland. Besides its role in regulating circadian rhythms, melatonin has a wide range of protective functions in the central nervous system (CNS) disorders. The mechanisms underlying this protective function are associated with the regulatory effects of melatonin on related genes and proteins. In addition to messenger ribonucleic acid (RNA) that can be translated into protein, an increasing number of non-coding RNAs in the human body are proven to participate in many diseases. This review discusses the current progress of research on the effects of melatonin modulation of non-coding RNAs (ncRNAs), including microRNA, long ncRNA, and circular RNA. The role of melatonin in regulating common pathological mechanisms through these ncRNAs is also summarized. Furthermore, the ncRNAs, currently shown to be involved in melatonin signaling in CNS diseases, are discussed. The information compiled in this review will open new avenues for future research into melatonin mechanisms and provide a further understanding of ncRNAs in the CNS.


2021 ◽  
Vol 17 (2) ◽  
pp. 6-15
Author(s):  
L.A. Dziak ◽  
O.S. Tsurkalenko ◽  
K.V. Chekha ◽  
V.M. Suk

Coronavirus infection is a systemic pathology resulting in impairment of the nervous system. The involvement of the central nervous system in COVID-19 is diverse by clinical manifestations and main mechanisms. The mechanisms of interrelations between SARS-CoV-2 and the nervous system include a direct virus-induced lesion of the central nervous system, inflammatory-mediated impairment, thrombus burden, and impairment caused by hypoxia and homeostasis. Due to the multi-factor mechanisms (viral, immune, hypoxic, hypercoagulation), the SARS-CoV-2 infection can cause a wide range of neurological disorders involving both the central and peripheral nervous system and end organs. Dizziness, headache, altered level of consciousness, acute cerebrovascular diseases, hypogeusia, hyposmia, peripheral neuropathies, sleep disorders, delirium, neuralgia, myalgia are the most common signs. The structural and functional changes in various organs and systems and many neurological symptoms are determined to persist after COVID-19. Regardless of the numerous clinical reports about the neurological and psychiatric symptoms of COVID-19 as before it is difficult to determine if they are associated with the direct or indirect impact of viral infection or they are secondary to hypoxia, sepsis, cytokine reaction, and multiple organ failure. Penetrated the brain, COVID-19 can impact the other organs and systems and the body in general. Given the mechanisms of impairment, the survivors after COVID-19 with the infection penetrated the brain are more susceptible to more serious diseases such as Parkinson’s disease, cognitive decline, multiple sclerosis, and other autoimmune diseases. Given the multi-factor pathogenesis of COVID-19 resulting in long-term persistence of the clinical symptoms due to impaired neuroplasticity and neurogenesis followed by cholinergic deficiency, the usage of Neuroxon® 1000 mg a day with twice-day dosing for 30 days. Also, a long-term follow-up and control over the COVID-19 patients are recommended for the prophylaxis, timely determination, and correction of long-term complications.


2019 ◽  
Vol 70 (10) ◽  
pp. 3579-3581

Zinc ions are considered to be one of the most abundant trace elements in the human body. Among many important functions, zinc ions regulate the function of numerous structural, transcriptional and enzymatic proteins that play important roles in the correct function of the central nervous system. Thus, in the present work we were interested in determining some preliminary relevance for the possible effect of acute zinc administration on the anxiety-like behavior. Our initial results described here are showing interesting biotechnological relevance for zinc in this anxiety-related context and also further theoretical developing on this area considering oxidative stress related mechanisms. Moreover, the cardiovascular relevance in both contexts of magnesium vs. cardiovascular effects or anxiety and its relations with the cardiovascular system are presented. Keywords: magnesium, anxiety, oxidative stress, cardiovascular


Sign in / Sign up

Export Citation Format

Share Document