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Pharmaceuticals
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Recent Advances in the Pharmacology of Serotonin and Its Receptors
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Recent Advances in the Pharmacology of Serotonin and Its Receptors

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

Deadline for manuscript submissions: 20 April 2024 | Viewed by 4921

Special Issue Editors

Dr. Karolina Pytka

E-Mail Website
Guest Editor
Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland
Interests: depression; cognition; biased agonists; drug discovery
Special Issues, Collections and Topics in MDPI journals
Dr. Elżbieta Żmudzka

E-Mail Website
Guest Editor
Department of Social Pharmacy, Jagiellonian University Medical College, Medyczna 9 St., 30-688 Kraków, Poland
Interests: pharmacology; behavioral testing; neuropsychopharmacology; behavioral neuroscience

Special Issue Information

Dear Colleagues,

Serotonin is one of the vital neurotransmitters in the central nervous system, as well as a hormone regulating a wide range of physiological functions. The multifunctioning of serotonin neurotransmission is involved in many diseases. The effects of serotonin through different serotonergic receptors are observed not only centrally in mood, sleep, memory, or anxiety control but also peripherally, e.g., in the modulation of the gastrointestinal tract. A thorough understanding of the molecular, physiological, and pharmacological basis of serotonin's action will undoubtedly allow a better understanding of the pathophysiology of many diseases and, thus, facilitate the search for new therapeutic targets connected with serotonin and its receptors.

In this Special Issue, we would like to bring together experts investigating serotonin and its receptors and invite them to present their recent results. We also welcome review articles and short communications on the latest achievements in this field

Dr. Karolina Pytka
Dr. Elżbieta Żmudzka
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

  • serotonin
  • serotonergic system
  • serotonergic receptors
  • serotonin neurotransmission
  • central nervous system
  • neuropsychiatry
  • neuropharmacology
  • peripheral serotonin
  • gastrointestinal tract
  • preclinical studies
  • clinical studies

Published Papers (3 papers)

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Research

13 pages, 1320 KiB  
Article
The Relationship between Character Traits and In Vivo Cerebral Serotonin Transporter Availability in Healthy Subjects: A High-Resolution PET Study with C-11 DASB
by Jeong-Hee Kim, Hang-Keun Kim, Sang-Wha Lee, Young-Don Son and Jong-Hoon Kim
Pharmaceuticals 2023, 16(5), 759; https://doi.org/10.3390/ph16050759 - 18 May 2023
Viewed by 990
Abstract
To elucidate the potential roles of serotonergic activity in human character traits (i.e., self-directedness, cooperativeness, and self-transcendence), we investigated the relationship between these character traits and serotonin transporter (5-HTT) in healthy subjects. Twenty-four participants underwent High-Resolution Research Tomograph–positron emission tomography scans with [ [...] Read more.
To elucidate the potential roles of serotonergic activity in human character traits (i.e., self-directedness, cooperativeness, and self-transcendence), we investigated the relationship between these character traits and serotonin transporter (5-HTT) in healthy subjects. Twenty-four participants underwent High-Resolution Research Tomograph–positron emission tomography scans with [11C]DASB. To quantify 5-HTT availability, binding potential (BPND) of [11C]DASB was obtained using the simplified reference tissue model. The Temperament and Character Inventory was used to assess subjects’ levels of three character traits. There were no significant correlations between the three character traits. Self-directedness was significantly positively correlated with [11C]DASB BPND in the left hippocampus, left middle occipital gyrus, bilateral superior parietal gyrus, left inferior parietal gyrus, left middle temporal gyrus (MTG), and left inferior temporal gyrus (ITG). Cooperativeness was significantly negatively correlated with [11C]DASB BPND in the median raphe nucleus. Self-transcendence was significantly negatively correlated with [11C]DASB BPND in the right MTG and right ITG. Our results show significant correlations between the three character traits and 5-HTT availability in specific brain regions. In particular, self-directedness was significantly positively correlated with 5-HTT availability, suggesting that a goal-oriented, self-confident, and resourceful character may be related to higher serotonergic neurotransmission. Full article
(This article belongs to the Special Issue Recent Advances in the Pharmacology of Serotonin and Its Receptors)
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21 pages, 1402 KiB  
Article
Novel Multimodal Salicylamide Derivative with Antidepressant-like, Anxiolytic-like, Antipsychotic-like, and Anti-Amnesic Activity in Mice
by Elżbieta Żmudzka, Klaudia Lustyk, Monika Głuch-Lutwin, Małgorzata Wolak, Jolanta Jaśkowska, Marcin Kołaczkowski, Jacek Sapa and Karolina Pytka
Pharmaceuticals 2023, 16(2), 175; https://doi.org/10.3390/ph16020175 - 24 Jan 2023
Cited by 1 | Viewed by 1543
Abstract
Depression, anxiety, and schizophrenia may coexist in psychiatric patients. Moreover, these disorders are very often associated with cognitive impairments. However, pharmacotherapy of these conditions remains challenging due to limited drug effectiveness or numerous side effects. Therefore, there is an urgent need to develop [...] Read more.
Depression, anxiety, and schizophrenia may coexist in psychiatric patients. Moreover, these disorders are very often associated with cognitive impairments. However, pharmacotherapy of these conditions remains challenging due to limited drug effectiveness or numerous side effects. Therefore, there is an urgent need to develop novel multimodal compounds that can be used to treat depression, anxiety, and schizophrenia, as well as memory deficits. Thus, this study aimed to evaluate the potential antidepressant-like, anxiolytic-like, antipsychotic-like effects, and anti-amnesic properties, of the novel arylpiperazine derivative of salicylamide, JJGW07, with an affinity towards serotonin 5-HT1A, 5-HT2A, and 5-HT7 and dopamine D2 receptors. Firstly, we investigated the compound’s affinity for 5-HT6 receptors and its functional activity by using in vitro assays. JJGW07 did not bind to 5-HT6 receptors and showed antagonistic properties for 5-HT1A, 5-HT2A, 5-HT7, and D2 receptors. Based on the receptor profile, we performed behavioral studies in mice to evaluate the antidepressant-like, anxiolytic-like, and antipsychotic-like activity of the tested compound using forced swim and tail suspension tests; four-plate, marble-burying, and elevated plus maze tests; and MK-801- and amphetamine-induced hyperlocomotion tests, respectively. JJGW07 revealed antidepressant-like properties in the tail suspension test, anxiolytic-like effects in the four-plate and marble-burying tests, and antipsychotic-like activity in the MK-801-induced hyperlocomotion test. Importantly, the tested compound did not induce catalepsy and motor impairments or influence locomotor activity in rodents. Finally, to assess the potential procognitive and anti-amnesic properties of JJGW07, we used passive avoidance and object recognition tests in mice. JJGW07 demonstrated positive effects on long-term emotional memory and also ameliorated MK-801-induced emotional memory impairments in mice, but showed no procognitive properties in the case of recognition memory. Our results encourage the search for new compounds among salicylamide derivatives, which could be model structures with multitarget mechanisms of action that could be used in psychiatric disorder therapy. Full article
(This article belongs to the Special Issue Recent Advances in the Pharmacology of Serotonin and Its Receptors)
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21 pages, 4258 KiB  
Article
Selective 5-HT6 Receptor Ligands (Agonist and Antagonist) Show Different Effects on Antipsychotic Drug-Induced Metabolic Dysfunctions in Rats
by Anna Partyka, Katarzyna Górecka, Joanna Gdula-Argasińska, Natalia Wilczyńska-Zawal, Magdalena Jastrzębska-Więsek and Anna Wesołowska
Pharmaceuticals 2023, 16(2), 154; https://doi.org/10.3390/ph16020154 - 20 Jan 2023
Viewed by 1485
Abstract
It is estimated that in patients taking antipsychotic drugs (APDs), metabolic syndrome occurs 2–3 times more often than in the general population. It manifests itself in abdominal obesity, elevated glucose concentration, and dyslipidemia. Despite the high prevalence of this disorder, only a small [...] Read more.
It is estimated that in patients taking antipsychotic drugs (APDs), metabolic syndrome occurs 2–3 times more often than in the general population. It manifests itself in abdominal obesity, elevated glucose concentration, and dyslipidemia. Despite the high prevalence of this disorder, only a small percentage of patients receive appropriate and effective treatment, and none of the available methods for preventing or treating APD-induced metabolic side effects is satisfactory. A promising supplement to antipsychotic therapy appears to be ligands of the serotonin 6 (5-HT6) receptor. The present study aimed to examine the chronic effects of the selected APDs (haloperidol, risperidone, olanzapine), administered alone and in combination with a selective 5-HT6 agonist (WAY-181187) or antagonist (SB-742457), on weight gain, food intake, serum lipid profile, glucose level, and a spectrum of hormones derived from adipose (leptin, adiponectin) and gastrointestinal (insulin, ghrelin) tissue in rats. SB-742457 inhibited increased weight gain and alleviated hyperglycemia induced by APDs more strongly than did WAY-181187, but also intensified dyslipidemia. WAY-181187 tended to improve the lipid profile, but increased the glucose level. The greatest benefits were obtained when WAY-181187 or SB-742457 were co-administered with haloperidol. It is difficult to assess whether the modification of the serum levels of insulin, leptin, ghrelin, and adiponectin depended on the treatment applied or other drug-independent factors; therefore, further research is needed. Full article
(This article belongs to the Special Issue Recent Advances in the Pharmacology of Serotonin and Its Receptors)
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