drug action
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Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 533
Author(s):  
Małgorzata Jarończyk ◽  
Jarosław Walory

Antidepressants target a variety of proteins in the central nervous system (CNS), the most important belonging to the family of G-protein coupled receptors and the family of neurotransmitter transporters. The increasing number of crystallographic structures of these proteins have significantly contributed to the knowledge of their mechanism of action, as well as to the design of new drugs. Several computational approaches such as molecular docking, molecular dynamics, and virtual screening are useful for elucidating the mechanism of drug action and are important for drug design. This review is a survey of molecular targets for antidepressants in the CNS and computer based strategies to discover novel compounds with antidepressant activity.


COVID ◽  
2022 ◽  
Vol 2 (1) ◽  
pp. 60-75
Author(s):  
Christine Chable-Bessia ◽  
Charlotte Boullé ◽  
Aymeric Neyret ◽  
Jitendriya Swain ◽  
Mathilde Hénaut ◽  
...  

Ivermectin was first approved for human use as an endectocide in the 1980s. It remains one of the most important global health medicines in history and has recently been shown to exert in vitro activity against SARS-CoV-2. However, the macrocyclic lactone family of compounds has not previously been evaluated for activity against SARS-CoV-2. The present study aims at comparing their anti-viral activity in relevant human pulmonary cell lines in vitro. Here, in vitro antiviral activity of the avermectins (ivermectin and selamectin) and milbemycins (moxidectin and milbemycin oxime) were assessed against a clinical isolate from a CHU Montpellier patient infected with SARS-CoV-2 in 2020. Ivermectin, like the other macrocyclic lactones moxidectin, milbemycin oxime and selamectin, reduced SARS-CoV-2 replication in vitro (EC50 of 2–5 μM). Immunofluorescence assays with ivermectin and moxidectin showed a reduction in the number of infected and polynuclear cells, suggesting a drug action on viral cell fusion. However, cellular toxicity of the avermectins and milbemycins during infection showed a very low selectivity index of <10. Thus, none of these agents appears suitable for human use for its anti-SARS-CoV-2 activity per se, due to low selectivity index.


2022 ◽  
pp. candisc.0212.2021
Author(s):  
Deborah Plana ◽  
Adam C Palmer ◽  
Peter K Sorger

Author(s):  
Chinnarao Pinisetti ◽  
Vimal Arora

Bio-enhancers are the compounds that enhance the bioavailability of active pharmaceutical ingredients without itself having any pharmacological action. Most of them are of natural origin and do not have any side effects. They enhance the bioavailability by influencing variety of mechanisms involved in the drug action like penetration enhancement, improving metabolism, enzyme inhibition, drug targeting etc. Use of these compounds help to reduce the dose frequency which in turn reduces drug retention in turn causing the toxicity and it also helps in developing cost-effective products. Present days these are widely used to enhance the bioavailability of anti-bacterial, anti-viral, antibiotic, anticancer, anti-inflammatory, cardiovascular drugs etc and effective drug targeting. The present review is designed to emphasize the importance of certain phytoconstituents working as bio-enhancers, their classification and different mechanisms of their activity.


2021 ◽  
Vol 15 ◽  
Author(s):  
Michael Colla ◽  
Hanne Scheerer ◽  
Steffi Weidt ◽  
Erich Seifritz ◽  
Golo Kronenberg

The serendipitous discovery of ketamine’s antidepressant effects represents one of the major landmarks in neuropsychopharmacological research of the last 50 years. Ketamine provides an exciting challenge to traditional concepts of antidepressant drug therapy, producing rapid antidepressant effects seemingly without targeting monoaminergic pathways in the conventional way. In consequence, the advent of ketamine has spawned a plethora of neurobiological research into its putative mechanisms. Here, we provide a brief overview of current theories of antidepressant drug action including monoaminergic signaling, disinhibition of glutamatergic neurotransmission, neurotrophic and neuroplastic effects, and how these might relate to ketamine. Given that research into ketamine has not yet yielded new therapies beyond ketamine itself, current knowledge gaps and limitations of available studies are also discussed.


2021 ◽  
Author(s):  
Samuel T. Slocum ◽  
Jeffrey F. DiBerto ◽  
Bryan L. Roth
Keyword(s):  

2021 ◽  
pp. 215-224
Author(s):  
Amy Z. Crepeau

Medications used in the treatment of nervous system disorders typically modulate neurotransmitter function or action potential propagation and alter neurologic function. This chapter reviews the principles of pharmacokinetics, the major targets for drug action to provide a basis for understanding how medications exert their action, and disease-specific treatments. An understanding of the pharmacokinetic principles of neurologic medications is important for prescribing and ordering medication. Multiple routes of administration, including intravenous, sublingual, intramuscular, subcutaneous, rectal, oral, and transdermal, are available for delivery of neurologic medications.


Author(s):  
Nitin Lavate

Pharmacology, the science of drug action, has helped to elucidate many basic physiological and pathological mechanisms in health and disease. Various animal experimental models have been designed to study the effect of drugs on living organisms and isolated tissues. These give an insight about where and how a drug acts, the mode of action of a drug, its effect on various body systems and probable adverse effects before administration of a drug. Therefore, the object of pharmacology is to provide such scientific data in animals as well as humans, which forms the basis of rational therapeutics. The  Jalamahabhuta is fundamental base of origin for kapha  dosha and mootra. These are supposed to have Asray-Asrayi Sambandha . It means these are directly proportional to each other. So by using the drug which is having the mootrala property Kapha may be controlled. Here an effort is made to prove this concept with modern parameters like immunomodulation, anti-inflammatory and antihistaminic activity.  


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