Triperidol was found to be a more potent 3H-dopamine uptake inhibitor than chlorpromazine in homogenates from rat striatum. Inhibition kinetics were competitive for triperidol and non-competitive for chlorpromazine. When drugs were given in vivo, d-amphetamine (10 mg/kg) blocked the 3H-dopamine uptake by about 50% whereas the neuroleptics did not modify the process even at highly sedating doses. Combined treatments with d-amphetamine and neuroleptics showed that only triperidol potentiated the blocking effect of d-amphetamine on 3-H-dopamine uptake. However, such a potentiation was not observed when triperidol and d-amphetamine were simultaneously added in vitro. The results tend to suggest that the postulated actions of neuroleptics on presynaptic sites in the striatum may be more important with the butyrophenone, triperidol than with the phenothiazine, chlorpromazine.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/0014-2999(76)90135-7 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mutations of tyrosine 467 in the human norepinephrine transporter attenuate HIV-1 Tat-induced inhibition of dopamine transport while retaining physiological function.
PLoS One
September 2022
Department of Drug Discovery and Biomedical Sciences, College of Pharmacy, University of South Carolina, Columbia, SC, United States of America.
Dysregulation of dopaminergic transmission induced by the HIV-1 transactivator of transcription (Tat) has been implicated as a central factor in the development of HIV-1 associated neurocognitive disorders (HAND). We have demonstrated that the tyrosine470 residue of the human dopamine transporter (hDAT) plays a critical role in Tat-hDAT interaction. Based on the computational modeling predictions, the present study sought to examine the mutational effects of the tyrosine467 residue of the human norepinephrine transporter (hNET), a corresponding residue of the hDAT tyrosine470, on Tat-induced inhibition of reuptake of dopamine through the hNET.
View Article and Find Full Text PDFA daily single dose of a novel modafinil analogue CE-123 improves memory acquisition and memory retrieval.
Behav Brain Res
May 2018
Department of Neuroproteomics, Paracelsus Medical University, Salzburg, Austria. Electronic address:
Article Synopsis
- CE-123, a modafinil analogue, effectively inhibits dopamine reuptake and is being studied for its potential to enhance memory performance in rats.
- In vitro tests showed CE-123 selectively blocked dopamine uptake while having minimal effects on serotonin and norepinephrine transporters.
- Behavioral studies indicated that CE-123 improved memory acquisition and retrieval in rats, which correlates with increased levels of certain dopamine receptors in key brain regions, suggesting a mechanism for its cognitive benefits.
Licochalcone A Prevents the Loss of Dopaminergic Neurons by Inhibiting Microglial Activation in Lipopolysaccharide (LPS)-Induced Parkinson's Disease Models.
Int J Mol Sci
September 2017
College of Animal Science and Veterinary Medicine, Jilin University, Changchun 130062, China.
Article Synopsis
- Licochalcone A (Lico.A), a flavonoid from licorice, shows potential neuroprotective effects in Parkinson's disease by reducing inflammation and protecting dopaminergic neurons.
- The study reveals that Lico.A inhibits microglial activation and the production of inflammatory mediators by blocking key signaling pathways in cell models.
- In vivo, Lico.A treatment in rat models mitigates microglial activation, prevents dopaminergic neuron loss, and improves behavioral deficits associated with Parkinson's disease.
Urinary Dopamine as a Potential Index of the Transport Activity of Multidrug and Toxin Extrusion in the Kidney.
Int J Mol Sci
July 2016
Department of Pharmacy, Kyushu University Hospital, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
Dopamine is a cationic natriuretic catecholamine synthesized in proximal tubular cells (PTCs) of the kidney before secretion into the lumen, a key site of its action. However, the molecular mechanisms underlying dopamine secretion into the lumen remain unclear. Multidrug and toxin extrusion (MATE) is a H⁺/organic cation antiporter that is highly expressed in the brush border membrane of PTCs and mediates the efflux of organic cations, including metformin and cisplatin, from the epithelial cells into the urine.
View Article and Find Full Text PDFLong Withdrawal of Methylphenidate Induces a Differential Response of the Dopaminergic System and Increases Sensitivity to Cocaine in the Prefrontal Cortex of Spontaneously Hypertensive Rats.
PLoS One
June 2016
Laboratório de Neurofarmacologia, Departamento de Fisiologia e Farmacologia, Instituto Biomédico, Universidade Federal Fluminense, Niterói, RJ, Brazil.
Methylphenidate (MPD) is one of the most prescribed drugs for alleviating the symptoms of Attention Deficit/Hyperactivity Disorder (ADHD). However, changes in the molecular mechanisms related to MPD withdrawal and susceptibility to consumption of other psychostimulants in normal individuals or individuals with ADHD phenotype are not completely understood. The aims of the present study were: (i) to characterize the molecular differences in the prefrontal dopaminergic system of SHR and Wistar strains, (ii) to establish the neurochemical consequences of short- (24 hours) and long-term (10 days) MPD withdrawal after a subchronic treatment (30 days) with Ritalin® (Methylphenidate Hydrochloride; 2.
View Article and Find Full Text PDFWant 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!