Overall, BZDs are generally classified according to their pharmacokinetic characteristics, i.e. Thus, the sedative, anterograde amnesic and anticonvulsant actions, as well as the addictive potential of these drugs, require the presence of α 1-containing GABA A receptors, while the anxiolytic effects are mediated by GABA A receptors containing α 2 subunits, and the myorelaxant actions by GABA A receptors containing α 2, α 3, and α 5 subunits. The pharmacological activity of BZDs is determined by the type of GABA A receptor α subunit to which they bind. These complex pharmacological activities explain the different clinical effects ( i.e., anxiolytic, hypnotic, anticonvulsant, amnestic, and muscle relaxant) of BZDs.
As a result, maximal currents elicited by GABA remain unaffected, and the GABA concentration channel opening curve is shifted to lower GABA concentrations’ chloride channel that hyperpolarizes the cell and accounts for GABA’s inhibitory effect throughout the central nervous system. This alteration, in turns, induces a conformational change in the GABA A receptor such as to increase the apparent affinity for channel gating by GABA at both agonist sites. BZDs bind to the pocket created by α and γ subunits and induce a conformational change in the GABA A receptor. The GABA A receptor is a ligand-gated chloride-selective ion channel build-up of five subunits: two α, two ß (the binding site for endogenous neurotransmitter) and one γ.
GABA represents the main inhibitor neurotransmitter in the brain and plays an important role in modulating the activity of many neurons, including those in the amygdala and prefrontal cortex. Mazzini”, ASL 4 Teramo, Italyīenzodiazepines (BZDs) act as positive allosteric modulators on the gamma-aminobutyric acid (GABA) A receptor. D’Annunzio”, Chieti, Italy 10NHS, Department of Mental Health, Psychiatric Service of Diagnosis and Treatment, Hospital “G. Marconi Telematic University, Rome, Italy 7Addictions Observatory (ODDPSS), Rome, Italy 8Mental Health Department - ASL Roma 2, Rome, Italy 9Department of Neuroscience, Imaging and Clinical Science, Chair of Psychiatry, University of “G. Katie Levinson, Credit Karma Ilya Levtov, Abigail Lubow, Vinson & Elkins LLP C Justine Macneil, Macneil Law Office Michelle Margolis, Discovery Behavioral Health Gideon Marks, Google Developers Launchpad Boris Maysel, Siklu Communication Mark Miller, Law Office of Mark E.1Psychopharmacology, Drug Misuse and Novel Psychoactive Substances Research Unit, School of Life and Medical Sciences, University of Hertfordshire, Hatfield, AL10 9AB, Herts, UK 2Department of Clinical Neurosciences/DIMSC, School of Medicine, Section of Psychiatry, Polytechnic University of Marche, Ancona, Italy 3Polyedra, Teramo, Italy 4Swansea University Medical School, Ysgol Feddygaeth Prifysgol Abertawe, UK 5NESMOS Department (Neurosciences, Mental Health and Sensory Organs), Sapienza University - Rome, School of Medicine and Psychology Sant’Andrea Hospital, Rome, Italy 6School of psychology - G. Oded Hermoni, J-Ventures & J-Angels Bruce Highman, Highman & Highman Jason Hitchcock, Twitch Shana Inspektor, Stradling Yocca Carlson & Rauth Sara Kaplan, Tailored Trainings Leslie Katz, Clark Hill Law Amanda Katzenstein, Salesforce Cary Kletter, Kletter Law Joshua Krafchin, Democracy Space Tali Krakowsky Apel, Facebook Erica Labovitz, Indiegogo Inc Warren Lazarow, O'Melveny & Myers Lacy Lefkowitz, Oakland Unified School Dst Marina Levi, Stealth AI Startup Karina Levitian, Lookout
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