Transporters of dopamine, serotonin, and norepinephrine have been empirically used as medication targets for several mental illnesses in the last decades. These protein-targeted medications are effective only for subpopulations of patients with transporter-related brain disorders. Since the cDNA clonings in early 1990s, molecular studies of these transporters have revealed a wealth of information about the transporters' structure-activity relationship (SAR), neuropharmacology, cell biology, biochemistry, pharmacogenetics, and the diseases related to the human genes encoding these transporters among related regulators. Such new information creates a unique opportunity to develop transporter-specific medications based on SAR, mRNA, DNA, and perhaps transporter trafficking regulation for a number of highly relevant diseases including substance abuse, depression, schizophrenia, and Parkinson's disease.
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http://dx.doi.org/10.1016/B978-0-12-385506-0.00001-6 | DOI Listing |
Expert Opin Pharmacother
December 2024
Department of Neurology, UTHealth Houston McGovern Medical School, Houston, TX, USA.
Introduction: Chorea is a motor manifestation of Huntington's disease (HD), which can lead to decreased functional independence and falls. Even though multiple classes of medications have been used to treat this symptom, only the vesicular monoamine transporter 2 (VMAT2) inhibitors tetrabenazine, deutetrabenazine, and valbenazine have been approved by the FDA for this indication.
Areas Covered: This article reviews the pharmacological properties, clinical efficacy, safety, and tolerability of valbenazine in the treatment of chorea in HD.
ACS Chem Neurosci
December 2024
Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, Cracow 30-688, Poland.
The sodium-dependent membrane transporter SLC6A15 (BAT2) belongs to the SLC6 family, which comprises carriers of amino acids and monoamines. BAT2 is expressed in the central nervous system (CNS), including the glutaminergic and GABAergic system. SLC6A15 supplies neurons with neutral amino acids.
View Article and Find Full Text PDFGeorgian Med News
October 2024
Institute of Translational Biomedicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.
Introduction: The annual growth of psychiatric and neurodegenerative diseases requires new therapeutic strategies for delivering active pharmaceutical molecules to the brain. Non-invasive intranasal drug delivery is a promising method that allows bypassing of the blood-brain barrier and the liver de-toxification system.
Results: The review discusses the main results of experimental studies of the effect of intranasal substances of amino acid and peptide nature on the monoamine systems of the brain.
Major depressive disorder (MDD) is one of the most common diseases affecting millions of people worldwide. The use of existing antidepressants in many cases does not allow achieving stable remission, probably due to insufficient understanding of pathological mechanisms. This indicates the need for the development of more effective drugs based on in-depth understanding of MDD's pathophysiology.
View Article and Find Full Text PDFNeuropharmacology
December 2024
- Department of Psychopharmacology, Valdman Institute of Pharmacology, Pavlov First Saint Petersburg State Medical University, Saint Petersburg, Russia. Electronic address:
Background: Apathy is a syndrome of decreased goal-directed activity, one of the main features of different brain disorders. Despite its high prevalence and life-threatening potential, there are currently very few options for its pharmacological treatment, which may be related to the lack of valid animal models.
Aims: The vesicular monoamine transporter 2 inhibitor tetrabenazine (TBZ) was used in this study to model apathy-related behavior in pathologies linked to a depletion of dopamine.
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