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)90243-5DOI Listing

Publication Analysis

Top Keywords

uptake monoamines
8
fusaric acid
8
uptake disulfiram
8
disulfiram fla
8
uptake
5
interference inhibitors
4
inhibitors dopamine-beta-hydroxylase
4
dopamine-beta-hydroxylase uptake
4
monoamines chromaffin
4
chromaffin granular
4

Similar Publications

Advances in Alzheimer's disease control approaches via carbon nanotubes.

Nanomedicine (Lond)

January 2025

Academy of Medical Engineering and Translational Medicine, Tianjin University, Tianjin, China.

Article Synopsis
  • Growing global concern about Alzheimer's disease (AD) stems from its earlier onset and economic impact, leading to neurodegeneration and loss of autonomy.
  • Carbon-based nanomaterials, particularly carbon nanotubes (CNTs), are gaining attention in AD research for their high biocompatibility and potential applications in drug delivery, biosensing, and molecular imaging.
  • CNTs can enhance AD treatment strategies by safely delivering drugs to the brain, detecting neurotransmitter levels, inhibiting harmful protein formation, and promoting regeneration in the central nervous system.
View Article and Find Full Text PDF

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 PDF

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 PDF

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 PDF
Article Synopsis
  • D6-[F]FP-(+)-DTBZ is a new imaging agent designed for PET scans that helps diagnose Parkinson's disease (PD) by tracking VMAT2 transporters in the brain.
  • In a study, this radioligand demonstrated efficient production, high purity, and distinct uptake in brain regions associated with PD, showing a greater effectiveness compared to its non-deuterated counterpart.
  • The findings suggest that D6-[F]FP-(+)-DTBZ could serve as a safer, more effective tool for monitoring VMAT2 levels in monoamine neurons, potentially improving PD diagnosis.
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!