9 documents found, page 1 of 1

In vitro permeability of MDPV across Caco-2 cells for assessment of intestinal ...

Background: Synthetic cathinones, such as 3,4-methylenedioxypyrovalerone (MDPV), are widely studied chiral psychoactive substances [1]. Enantioselectivity studies on the toxicokinetic of synthetic cathinones are still scarce [2], namely on their ability to cross the intestinal membrane, which was evaluated only for methylone and pentedrone [3]. To isolate enantiomers for these studies, liquid chromatography (LC...

New 8-hydroxyquinoline derivatives as promising therapeutic approaches targetin...

Background: Alzheimer's disease, Parkinson's disease, and Amyotrophic lateral sclerosis are recognized as the most prevalent neurodegenerative diseases (NDs), presenting a huge burden for society. These diseases share common pathophysiological mechanisms, such oxidative stress, dysfunction in iron metabolism, ferroptosis, and protein misfolding [1-4]. Given their powerful metal chelating and antioxidant propert...

In silico study of (thio)xanthones-mediated P-glycoprotein activation

Background: P-glycoprotein (P-gp) is an efflux transporter located at the apical membrane of important barrier tissues, playing a crucial role in the detoxification of endobiotics and xenobiotics [1]. (Thio)xanthonic derivatives have been shown to be able of activating P-gp without increasing its expression, promoting an immediate increase in the amount of transported substrates. Thus, P-gp activation limits th...

Mechanisms behind the neurotoxicity of 2C-I and 25I-NBOMe drugs

Background: New Psychoactive Substances (NPS) pose significant health and legal risks worldwide. At the end of 2021, the European Monitoring Centre for Drugs and Drug Addiction was monitoring 886 NPS, 106 of them phenethylamines [1]. Phenethylamine derivatives include 2,5-dimethoxyphenethylamine-based (2C) and N-benzylphenethylamine-based (NBOMe) drugs, widely known for their psychedelic effects. However, their...

Antifungal activity of a new derivative of 5-aminoimidazole-4-carbohydrazonamide

[Excerpt] Fungal infections, as recognized by the World Health Organization (WHO), are among the most worrying challenges for the medical community due to their high incidence, recurrence, and the emergence of resistance to the few available drugs and therapies. The discovery of new molecules with antifungal activity, exhibiting new mechanisms of action and less side effects, thus represents an important step f...

Synergistic activity of a novel class of azoimidazole dyes with polyvinylpyrrol...

The high demand for novel antimicrobial textiles by the medical, health care, hygiene, sportswear, personal protective equipment, and filtration sectors promoted the growth of functional textiles. However, the efficacy of antimicrobial agents against different pathogens is a considerable challenge due to the distinctive mechanisms of action and resistance. The development of novel synergistic antimicrobial agen...

Toxicity of synthetic cathinones in human kidney (HK-2) cells

Mephedrone

Simultaneous determination of amphetamine derivatives in human urine after SPE ...

Amphetamine derivatives are a class of compounds increasingly abused as recreational drugs in various regions of the world. Although d-amphetamine (AMPH) and 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) are among the most commonly used, the abuse of other designer drugs such as 4-bromo-2,5-dimethoxyphenethylamine (2C-B) and 4-methylthioamphetamine (4-MTA) and their involvement in acute intoxications has be...