scholarly journals Pharmacological activities, mechanisms of action, and safety of salidroside in the central nervous system

2018 ◽  
Vol Volume 12 ◽  
pp. 1479-1489 ◽  
Author(s):  
Zhifeng Zhong ◽  
Jing Han ◽  
Jizhou Zhang ◽  
Qing Xiao ◽  
Juan Hu ◽  
...  
1979 ◽  
Vol 57 (7) ◽  
pp. 1014-1018 ◽  
Author(s):  
Sylvie Bouchard ◽  
Andrée G. Roberge

Biochemical properties and kinetic parameters of nonpurified dihydroxyphenylaianine –5-hydroxytryptophan decarboxylase extracted from brain and two peripheral organs, liver and adrenals, were studied in the cat. This study shows that decarboxylase activity in brain is lower than in peripheral organs and that 5-hydroxytryptophan can be decarboxylated without exogenous addition of pyridoxal-5′-phosphate (PLP). However, the addition of PLP substantially increases the enzyme activity. Excess of coenzyme (>60 μM) induces inhibition in adrenals and liver but not in the central nervous system (CNS). The observed inhibition might be related to the presence of a tetrahydroisoquinoline derivative formed in the medium. Differentiation between mechanisms of action of decarboxylase in the CNS and peripheral organs is suggested.


2009 ◽  
Vol 1;12 (1;1) ◽  
pp. 269-280
Author(s):  
Howard Smith

Despite nearing the end of the decade of pain research, the analgesic mechanisms of one of the most widely used and popular analgesics remains uncertain. Acetaminophen (APAP) (paracetamol [PARA]) has been used clinically for over a half of a century and although clinicians seem to be comfortable with its benefits, risks, and limitations, they still remain in the dark as to precisely what is providing its pain relief. What does seem clearer is that the predominant mechanisms of APAP’s analgesic effects are in the central nervous system (CNS). Although, which central effects are largely responsible for APAP’s effects on pain continue to be uncertain. Perhaps, the most accepted theory is that of APAP’s positive effects on the serotonergic descending inhibitory pathways. However, interactions with opioidergic systems, eicosanoid systems, and/or nitric oxide containing pathways may be involved as well. Furthermore, endocannabinoid signaling may play a role in APAP’s activation of the serotonergic descending inhibitory pathways. A greater understanding of APAP’s analgesic mechanisms may promote optimal utilization of analgesic polypharmacy. Key words: Acetaminophen (APAP), paracetamol (PARA), pain, analgesia, mechanisms of action, serotonin, opioids, endocannabinoids


2021 ◽  
Author(s):  
Antonio Wlisses da Silva ◽  
Maria Kueirislene A. Ferreira ◽  
Emanuela L. Rebouças ◽  
Francisco Rogenio S. Mendes ◽  
Atilano Lucas dos S. Moura ◽  
...  

Abstract Benzodiazepines are highly effective in combating anxiety; however, they have considerable adverse effects, so it is important to discover new safe anxiolytic agents. This study was designed to investigate the anxiolytic and anticonvulsant effect of natural product 2-hydroxy-3,4,6-trimethoxyacetophenone (HTMCX) and its possible mechanisms of action in adult zebrafish. The open field and light / dark tests (n = 6 animals/group) were used to assess anxiety and pentylenetetrazole (PTZ) as a seizure inducer. The 96-hour acute toxicity of HTMCX was also investigated. HTMCX (1, 3, and 10 mg / kg; v.o.) was not toxic and affected locomotor activity. The highest doses (3 and 10 mg / kg; v.o.) produced signs of anxiolytic action in the light / dark test, and this effect was abolished by the pizotifen (antagonist 5HTR1 and 5HTR2A / 2C), having the potential to form a complex in the same region of the site indicating that the anxiolytic effect via the serotonergic mechanism. However, the anxiolytic effect of HTMCX has not been abolished by flumazenil (antagonist GABARA), cyproheptadine (antagonist 5HTR2A), and granisetron (antagonist 5HTR3A / 3B). Therefore, HTMCX demonstrated an anxiolytic effect, suggesting that the 5HTR1 and 5HTR / 2C receptors may be involved in the pharmacological performance of this acetophenone in the central nervous system.


2021 ◽  
Vol 10 (12) ◽  
pp. e216101220479
Author(s):  
Patrícia e Silva Alves ◽  
Felipe Pereira da Silva Santos ◽  
Ana Paula Rodrigues ◽  
Leandro Sousa Dias ◽  
Giovanna Carvalho da Silva ◽  
...  

Due to the continuous increase in incidents of diseases and disorders in the central nervous system as neurodegenerative disease, the growth of studies that seek to use herbal medicines has been observed, since these are more easily produced and more economically viable, in addition to having side effects to a lesser extent when compared to existing synthetic drugs. In this way, a wide variety of plants have been analyzed for their medicinal purposes and this review presents papers published from 1970 to 2021 that describe the chemical composition pharmacological activities and elucidates mechanisms of action in the central nervous system (CNS) of the species Piper methysticum (Kava-kava). The Kava-kava has a class of compounds that include tannins, alkaloids, benzoic acid, cinnamic acid, sugars, bornyl-cinnamate, stigmasterol, flavocavaines, mucilages, pyrones, tetrahydroiangonins, phytochemicals that are responsible for the pharmacological activities of this plant being thus more studied as anxiolytic, sedative and neuroprotection. Some action mechanisms that describe the performance of kava in the CNS were also addressed, Being the main ones related to blocking of sodium and calcium ion channels, modulation of the erythroid 2 pathway, to receptors such as γ-aminobutyric acid, glutamatergics, glycine and cannabinoid, as well as monoamine oxidase and acetylcholinesterase enzymes, in addition to neurotransmitters such as dopamine, serotonin and norepinephrine. Therefore, this study aims to open new paths for more in-depth pharmacological studies on Kava-kava, and its use in the central nervous system.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 106 ◽  
Author(s):  
Maria Bonferoni ◽  
Luca Ferraro ◽  
Barbara Pavan ◽  
Sarah Beggiato ◽  
Elena Cavalieri ◽  
...  

The pharmacological activities of geraniol include anticancer and neuroprotective properties. However, its insolubility in water easily induces separation from aqueous formulations, causing administration difficulties. Here we propose new emulsified formulations of geraniol by using the amphiphilic polymer chitosan-oleate (CS-OA) as surfactant to combine mucoadhesive and absorption enhancer properties with stabilization effects on the oil dispersion. The formulation based on CS-OA 2% (w/w) (G-CS-OA-2.0%) showed viscosity values compatible with oral and nasal administration to rats, and mean diameter of the dispersed phase of 819 ± 104 nm. G-CS-OA-2.0% oral administration sensibly increases the geraniol bioavailability with respect to coarse emulsions obtained without CS-OA (AUC values in the bloodstream were 42,713 ± 1553 µg∙mL−1∙min and 2158 ± 82 µg∙mL−1∙min following administration of 50 mg/kg or 1 mg/kg, respectively), and enhances the aptitude of geraniol to reach the central nervous system from the bloodstream (AUC values in the cerebrospinal fluid were 7293 ± 408 µg∙mL−1∙min and 399 ± 25 µg∙mL−1∙min after oral administration of 50 mg/kg or 1 mg/kg, respectively). Moreover, relevant geraniol amounts were detected in the cerebrospinal fluid following the G-CS-OA-2% nasal administration (AUC values in the cerebrospinal fluid were 10,778 ± 477 µg∙mL−1∙min and 5571 ± 290 µg∙mL−1∙min after nasal administration of 4 mg/kg or 1 mg/kg, respectively).


Author(s):  
György Buzsáki ◽  
Fred H. Gage

ABSTRACT:This review summarizes the range of possible mechanisms of action of neuronal grafts in the central nervous system. It aims to illustrate the capacity and limitations of the transplanted tissue in the promotion of neurological recovery after experimental surgical insults.


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