Disulfiram and bis-(4-methyl-1-homopiperazinylthiocarbonyl)-disulphide (FLA 63) markedly inhibited the Mg2+/ATP-dependent uptake of various monoamines, e.g. dopamine (DA), by isolated membranes of bovine adrenal chromaffin granules. Both compounds affected DA-beta-hydroxylase (DBH) activity more markedly than the uptake of DA. Other inhibitors of DBH, e.g. fusaric acid and diethyldithiocarbaminate (DDC), did not interfere with DA uptake. Disulfiram and FLA 63, in contrast to fusaric acid and DDC, also caused a partial inhibition of Mg2+-dependent ATPase. It is concluded that the inhibition of monoamine uptake by disulfiram and FLA 63 is not related to their effect on DBH.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/0014-2999(75)90243-5 | DOI Listing |
Nanomedicine (Lond)
January 2025
Academy of Medical Engineering and Translational Medicine, Tianjin University, Tianjin, China.
Front Pharmacol
October 2024
Department of Biomedical Sciences, School of Medicine, City University of New York, New York, NY, United States.
Dopamine stimulates CDP-diacylglycerol biosynthesis through D-like receptors, particularly the D subtype most of which is intracellularly localized. CDP-diacylglycerol regulates phosphatidylinositol-4,5-bisphosphate-dependent signaling cascades by serving as obligatory substrate for phosphatidylinositol biosynthesis. Here, we used acute and organotypic brain tissues and cultured cells to explore the mechanism by which extracellular dopamine acts to modulate intracellular CDP-diacylglycerol.
View Article and Find Full Text PDFClin Nucl Med
December 2024
From the Department of Neurological Surgery, Faculty of Medicine, Kagawa University.
A teenager who suffered from left hemiparesis after traumatic brain injury underwent 18F-THK5351 PET 48, 286, and 810 days after the injury. The first scan showed slight uptake in the right corticospinal tract (CST), and the second scan showed intense uptake along the CST, which was significantly reduced in the third scan. The hemiparesis has improved between the first and second scans.
View Article and Find Full Text PDFBiol Pharm Bull
October 2024
Faculty of Pharmaceutical Sciences, Teikyo University.
Mesoridazine and metoclopramide are cationic drugs that are distributed in the human brain despite being substrates of multidrug resistance protein 1 (MDR1), an efflux transporter expressed at the blood-brain barrier (BBB). We investigated their transport mechanisms at the BBB using hCMEC/D3, a human cerebral microvascular endothelial cell line often used as an in vitro BBB model. The cells exhibited time- and concentration-dependent uptake of mesoridazine and metoclopramide, with K values of 34 and 277 µM, respectively.
View Article and Find Full Text PDFEJNMMI Radiopharm Chem
October 2024
Department of Nuclear Medicine, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, 510120, Guangdong, China.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!