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Dopamine, Histamine, Serotonin—Receptors, Ligands and Their Biological Role in Central Nervous System Diseases, 2nd Edition

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Neurobiology".

Deadline for manuscript submissions: 30 June 2024 | Viewed by 448

Special Issue Editors


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Guest Editor
Chair of Technology and Biotechnology of Medical Remedies, Faculty of Pharmacy, Jagiellonian University Medical College in Kraków, Ul. Medyczna 9, 30-688 Kraków, Poland
Interests: medicinal chemistry; multitarget ligands; drug design; synthesis; neurodegenerative disorders; histamine H3 receptors
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Hormone Biochemistry, Faculty of Medicine, Medical University of Lodz, Żeligowskiego 7/9 Str., 90-752 Lodz, Poland
Interests: neurodegeneration; CNS diseases; Alzheimer's disease; Parkinson's disease; novel treatments for CNS diseases; neuroprotective agents; dual targeting drugs; multi-targeting drugs; histamine; histamine receptors; biogenic amines
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The human brain, with its network of neurotransmitters, is still an intriguing mystery to us. Neurotransmitters direct the work of the entire brain, transmitting important information and influencing important vital functions.

Dopamine and serotonin are some of the most important neurotransmitters in our brain. The role of histamine is equally important in the sleep-wake cycle or in processes related to memory and concentration. Each of these amines, acting through their receptors, influences many important vital functions and plays an important role in the onset and course of many CNS diseases.

An in-depth knowledge and understanding of the mechanisms of these diseases onset and progression, especially those with an important role for dopamine, histamine or serotonin, can help identify early symptoms of them, and introduction of a proper therapy.

Papers on these amines, their receptors and ligands are encouraged. Particularly works involving the search for new active compounds, especially those with multitargeting activity, and their pharmacological or pharmacokinetic evaluation. All preclinical studies (including in vitro, ex vivo and in vivo studies) related to effects via dopamine, histamine or serotonin are welcome.

Dr. Dorota Łażewska
Dr. Anna Stasiak
Guest Editors

Manuscript Submission Information

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Keywords

  • biogenic amines (histamine, dopamine, serotonin)
  • receptors
  • ligands
  • antagonist/inverse agonist
  • affinity
  • intrinsic activity
  • multitarget ligands
  • molecular modeling
  • CNS diseases
  • neurodegeneration
  • psychiatric disorders
  • pain
  • in vitro studies
  • in silico studies
  • in vivo studies

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Published Papers (1 paper)

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Research

14 pages, 1340 KiB  
Article
Kinetic Properties and Pharmacological Modulation of High- and Low-Affinity Dopamine Transport in Striatal Astrocytes of Adult Rats
by Vesna Sočan, Klemen Dolinar and Mojca Kržan
Int. J. Mol. Sci. 2024, 25(10), 5135; https://doi.org/10.3390/ijms25105135 - 9 May 2024
Viewed by 216
Abstract
Astrocytes actively participate in neurotransmitter homeostasis by bidirectional communication with neuronal cells, a concept named the tripartite synapse, yet their role in dopamine (DA) homeostasis remains understudied. In the present study, we investigated the kinetic and molecular mechanisms of DA transport in cultured [...] Read more.
Astrocytes actively participate in neurotransmitter homeostasis by bidirectional communication with neuronal cells, a concept named the tripartite synapse, yet their role in dopamine (DA) homeostasis remains understudied. In the present study, we investigated the kinetic and molecular mechanisms of DA transport in cultured striatal astrocytes of adult rats. Kinetic uptake experiments were performed using radiolabeled [3H]-DA, whereas mRNA expression of the dopamine, norepinephrine, organic cation and plasma membrane monoamine transporters (DAT, NET, OCTs and PMAT) and DA receptors D1 and D2 was determined by qPCR. Additionally, astrocyte cultures were subjected to a 24 h treatment with the DA receptor agonist apomorphine, the DA receptor antagonist haloperidol and the DA precursor L-DOPA. [3H]-DA uptake exhibited temperature, concentration and sodium dependence, with potent inhibition by desipramine, nortriptyline and decynium-22, suggesting the involvement of multiple transporters. qPCR revealed prominent mRNA expression of the NET, the PMAT and OCT1, alongside lower levels of mRNA for OCT2, OCT3 and the DAT. Notably, apomorphine significantly altered NET, PMAT and D1 mRNA expression, while haloperidol and L-DOPA had a modest impact. Our findings demonstrate that striatal astrocytes aid in DA clearance by multiple transporters, which are influenced by dopaminergic drugs. Our study enhances the understanding of regional DA uptake, paving the way for targeted therapeutic interventions in dopaminergic disorders. Full article
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