Molecular and Toxicological Profiling of Drugs of Abuse—in Honor of Professor Félix Carvalho

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Molecular Medicine".

Deadline for manuscript submissions: 31 December 2024 | Viewed by 1268

Special Issue Editors


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UCIBIO, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: molecular toxicology; developmental neurotoxicology; new psychoactive substances; cannabinoids; oxidative stress
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UCIBIO, REQUIMTE, Laboratory of Toxicology, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
Interests: Cardiotoxicity; cardio-oncology; chemobrain; clinical toxicology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to this Special Issue that we have launched in honor of Prof. Félix Carvalho for his lifelong scientific, social and educational contributions to the field of drugs of abuse. He is a Full Professor in Toxicology and the former President of the Federation of European Toxicologists & European Societies of Toxicology (EUROTOX), who has dedicated over 25 years of his career to unraveling the toxicological profiling of substances of abuse, assessing the mechanistic signatures of pharmacologically active drugs. His expertise in mechanistic toxicology has directly resulted in the development of antidotes and therapeutics, repurposed from already existing drugs, against toxic agents or disorders with high public health impact worldwide due to their high morbidity and mortality levels. He is a scientific advisor on several national/international boards of regulatory agencies, as well as a Member of the Scientific Committee of the European Monitoring Center for Drugs and Drug Addiction (EMCDDA), External Expert of the European Medicines Agency (EMA), and Member of the Committee for Evaluation of Medicines at the National Authority of Medicines and Health Products, I.P. (INFARMED).

The monitoring of substance use worldwide highlights a pandemic with profound social, health, and economic consequences, as the latest 2023 World Drug Report estimates that almost 300 million people worldwide have used substances of abuse during 2021, an increase of about 23% over 10 years. Despite their collective impact on the central nervous system, these substances significantly differ in their neurochemical processes, addictive tendencies, and overall health effects, and also toxicologically impact other organ systems (e.g., respiratory, cardiovascular, liver, and kidneys). Understanding the mechanisms underlying the toxicological effects of these substances of abuse is thus highly important for researchers, clinicians, and policy-makers to (1) ascertain their addictive potential and the mechanisms that lead to adverse health consequences, (2) uncover new and/or improved approaches for intoxication treatments and rehabilitation, and (3) take better informed regulatory decisions.

This Special Issue aims to collect original research articles and reviews on the molecular aspects of different drugs of abuse, investigating their pharmacological and toxicological impacts on the brain and other organs.

We look forward to receiving your contributions.

Dr. João Pedro Silva
Dr. Vera Marisa Costa
Guest Editors

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Keywords

  • toxicodynamic
  • toxicokinetic
  • amphetamine-type stimulants, cannabis and cannabinoids, cocaine, hallucinogens, new psychoactive substances, opioids
  • immune modulation

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Published Papers (1 paper)

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Research

15 pages, 2522 KiB  
Article
Synthesis, Analytical Characterization, and Human CB1 Receptor Binding Studies of the Chloroindole Analogues of the Synthetic Cannabinoid MDMB-CHMICA
by Sascha Münster-Müller, Steven Hansen, Tobias Lucas, Arianna Giorgetti, Lukas Mogler, Svenja Fischmann, Folker Westphal, Volker Auwärter, Michael Pütz and Till Opatz
Biomolecules 2024, 14(11), 1414; https://doi.org/10.3390/biom14111414 - 6 Nov 2024
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Abstract
Synthetic cannabinoids (SCs) are one of the largest groups of new psychoactive substances (NPSs). However, the relationship between their chemical structure and the affinity to human CB1 receptors (hCB1), which mediates their psychotropic activity, is not well understood. Herein, the [...] Read more.
Synthetic cannabinoids (SCs) are one of the largest groups of new psychoactive substances (NPSs). However, the relationship between their chemical structure and the affinity to human CB1 receptors (hCB1), which mediates their psychotropic activity, is not well understood. Herein, the synthesis of the 2-, 4-, 5-, 6- and 7-chloroindole analogues of the synthetic cannabimimetic MDMB-CHMICA, along with their analytical characterization via ultraviolet–visible (UV/VIS), infrared (IR), nuclear magnetic resonance (NMR) spectroscopy, and mass spectrometry, is described. Furthermore, all five derivatives of MDMB-CHMICA were analyzed for their hCB1 binding affinities. Chlorination at position 4 and 5 of the indole core reduced the binding affinity compared to MDMB-CHMICA, while the test compounds chlorinated in positions 2, 6, and 7 largely retained their binding affinities relative to the non-chlorinated parent compound. Full article
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