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Pharmaceuticals
Special Issues
Sigma Receptors: Past, Present and Perspectives on Multiple Therapeutic Exploitations
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Sigma Receptors: Past, Present and Perspectives on Multiple Therapeutic Exploitations

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: closed (31 March 2024) | Viewed by 1300

Special Issue Editors

Dr. Katarzyna Szczepanska

E-Mail Website
Guest Editor
1. Department of Medicinal Chemistry, Institute of Pharmacology Polish Academy of Sciences, Kraków, Poland
2. Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland
Interests: medicinal chemistry; sigma-1 receptor ligands; histamine H3 receptor ligands; pain management
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Katarzyna Kiec-Kononowicz

E-Mail Website
Guest Editor
Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College in Kraków, Medyczna 9, 30-688 Kraków, Poland
Interests: medicinal chemistry; organic chemistry; drug discovery; GPCR ligands; sigma-1 receptor ligands

Special Issue Information

Dear Colleagues,

Sigma (σ) receptors, initially described as a subtype of opioid receptors, are now considered a separate class. Pharmacological studies have distinguished two types of σ receptors, namely σ1 and σ2. The sigma receptors have been implicated in a large number of apparently diverse conditions, including addiction, depression, pain, neurodegenerative conditions, cancer, and amyolateral sclerosis (among others), suggesting that their pharmacological regulation will yield useful drugs to treat several conditions.

The journal Pharmaceuticals invites both reviews and original articles that shed light on the challenges and opportunities of using Sigma receptors in drug discovery. Topics include the following: the design and synthesis of novel sigma-1 and sigma-2 receptor ligands, structure–activity relationship analysis, selective or multi-target-directed ligands that bind to sigma receptors, functional activity and the therapeutic potential of sigma receptors (state of the art and perspectives). The collection of manuscripts will be published as a Special Issue of the journal.

Dr. Katarzyna Szczepanska
Prof. Dr. Katarzyna Kiec-Kononowicz
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • sigma (σ) receptors
  • sigma (σ) receptors ligands
  • synthesis
  • structure-activity relationship analysis
  • functional activity
  • multiple therapeutic exploitations

Published Papers (1 paper)

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Review

22 pages, 4174 KiB  
Review
[18F]Fluspidine—A PET Tracer for Imaging of σ1 Receptors in the Central Nervous System
by Friedrich-Alexander Ludwig, Erik Laurini, Judith Schmidt, Sabrina Pricl, Winnie Deuther-Conrad and Bernhard Wünsch
Pharmaceuticals 2024, 17(2), 166; https://doi.org/10.3390/ph17020166 - 28 Jan 2024
Viewed by 1022
Abstract
σ1 receptors play a crucial role in various neurological and neurodegenerative diseases including pain, psychosis, Alzheimer’s disease, and depression. Spirocyclic piperidines represent a promising class of potent σ1 receptor ligands. The relationship between structural modifications and σ1 receptor affinity and [...] Read more.
σ1 receptors play a crucial role in various neurological and neurodegenerative diseases including pain, psychosis, Alzheimer’s disease, and depression. Spirocyclic piperidines represent a promising class of potent σ1 receptor ligands. The relationship between structural modifications and σ1 receptor affinity and selectivity over σ2 receptors led to the 2-fluoroethyl derivative fluspidine (2, Ki = 0.59 nM). Enantiomerically pure (S)-configured fluspidine ((S)-2) was prepared by the enantioselective reduction of the α,β-unsaturated ester 23 with NaBH4 and the enantiomerically pure co-catalyst (S,S)-24. The pharmacokinetic properties of both fluspidine enantiomers (R)-2 and (S)-2 were analyzed in vitro. Molecular dynamics simulations revealed very similar interactions of both fluspidine enantiomers with the σ1 receptor protein, with a strong ionic interaction between the protonated amino moiety of the piperidine ring and the COO- moiety of glutamate 172. The 18F-labeled radiotracers (S)-[18F]2 and (R)-[18F]2 were synthesized in automated syntheses using a TRACERlab FX FN synthesis module. High radiochemical yields and radiochemical purity were achieved. Radiometabolites were not found in the brains of mice, piglets, and rhesus monkeys. While both enantiomers revealed similar initial brain uptake, the slow washout of (R)-[18F]2 indicated a kind of irreversible binding. In the first clinical trial, (S)-[18F]2 was used to visualize σ1 receptors in the brains of patients with major depressive disorder (MDD). This study revealed an increased density of σ1 receptors in cortico-striato-(para)limbic brain regions of MDD patients. The increased density of σ1 receptors correlated with the severity of the depressive symptoms. In an occupancy study with the PET tracer (S)-[18F]2, the selective binding of pridopidine at σ1 receptors in the brain of healthy volunteers and HD patients was shown. Full article
(This article belongs to the Special Issue Sigma Receptors: Past, Present and Perspectives on Multiple Therapeutic Exploitations)
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