Electrochemical measurements using voltammetry or amperometry at carbon-fiber microelectrodes have been used in vitro and in vivo to examine regulatory mechanisms for the central dopamine system. In many of these experiments, dopamine efflux concentrations under control conditions are determined followed by their alterations in response to a drug treatment. The present study demonstrates that some drugs can affect dopamine measurements, not only by their expected pharmacological action but also by directly altering the microelectrode responsivity. The commonly used reuptake inhibitors GBR 12909 (10 microM) and nomifensine (5 microM) drastically reduce electrode sensitivity and, in the case of nomifensine, increase the time to reach a plateau in response to dopamine boluses (i.e. reduced 'frequency response'). Cocaine (10 microM) and WIN 35428 (2 microM) have negligible effect on these indices. This decrease in sensitivity was found in both nafion and non-nafion coated electrodes. Further, the reduction in sensitivity seen in non-nafion coated electrodes was not prevented by increasing the reversal potential (from +1.0 to +1.3 V) and voltage scan rate (from 350 to 450 V/s). These data suggest that care must be taken when interpreting data from voltammetric or amporometric experiments using carbon electrodes where GBR 12909 or nomifensine are used, especially at high concentrations. Furthermore, wherever possible, direct effects of a drug on electrode sensitivity and frequency response should be determined.
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Behav Brain Res
February 2025
Laboratory of Experimental Neuropsychobiology, Department of Biochemistry and Molecular Biology, Natural and Exact Sciences Center, Federal University of Santa Maria, 1000 Roraima Avenue, Santa Maria, RS 97105-900, Brazil; Graduate Program in Biological Sciences: Toxicological Biochemistry, Federal University of Santa Maria, 1000 Roraima Avenue, Santa Maria, RS 97105-900, Brazil; The International Zebrafish Neuroscience Research Consortium (ZNRC), 309 Palmer Court, Slidell, LA 70458, USA. Electronic address:
J Antibiot (Tokyo)
January 2025
School of Biosciences, University of Birmingham, Birmingham, B15 2TT, UK.
Mycobacterium tuberculosis is a bacterial pathogen, responsible for approximately 1.3 million deaths in 2022 through tuberculosis infections. The complex treatment regimen required to treat tuberculosis and growing rates of drug resistance, necessitates the development of new anti-mycobacterial agents.
View Article and Find Full Text PDFNature
August 2024
Key Laboratory of Biomacromolecules (CAS), National Laboratory of Biomacromolecules, CAS Center for Excellence in Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, Beijing, China.
The dopamine transporter has a crucial role in regulation of dopaminergic neurotransmission by uptake of dopamine into neurons and contributes to the abuse potential of psychomotor stimulants. Despite decades of study, the structure, substrate binding, conformational transitions and drug-binding poses of human dopamine transporter remain unknown. Here we report structures of the human dopamine transporter in its apo state, and in complex with the substrate dopamine, the attention deficit hyperactivity disorder drug methylphenidate, and the dopamine-uptake inhibitors GBR12909 and benztropine.
View Article and Find Full Text PDFBr J Pharmacol
August 2024
Department of Biomedicine, Pulmonary and Cardiovascular Pharmacology, Aarhus University, Aarhus, Denmark.
Background And Purpose: An estimated 40% of patients with erectile dysfunction have a poor prognosis for improvement with currently available treatments. The present study investigated whether a newly developed monoamine transport inhibitor, IP2015, improves erectile function.
Experimental Approach: We investigated the effects of IP2015 on monoamine uptake and binding, erectile function in rats and diabetic mice and the effect on corpus cavernosum contractility.
Nat Cancer
March 2024
Nash Family Department of Neuroscience, Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.
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