Academic Journal
Multitarget-Directed Ligands Hitting Serotonin Receptors: A Medicinal Chemistry Survey
| Title: | Multitarget-Directed Ligands Hitting Serotonin Receptors: A Medicinal Chemistry Survey |
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| Authors: | Imane Ghafir El Idrissi, Angela Santo, Enza Lacivita, Marcello Leopoldo |
| Source: | Pharmaceuticals, Vol 17, Iss 9, p 1238 (2024) |
| Publisher Information: | MDPI AG, 2024. |
| Publication Year: | 2024 |
| Collection: | LCC:Medicine LCC:Pharmacy and materia medica |
| Subject Terms: | serotonin, acetyl cholinesterases, butyryl cholinesterases, sigma receptors, multitarget-directed ligands, schizophrenia, Medicine, Pharmacy and materia medica, RS1-441 |
| More Details: | Serotonin (5-hydroxytryptamine, 5-HT) is a ubiquitous neurotransmitter in the human body. In the central nervous system, 5-HT affects sleep, pain, mood, appetite, and attention, while in the peripheral nervous system, 5-HT modulates peristalsis, mucus production, and blood vessel dilation. Fourteen membrane receptors mediate 5-HT activity. In agreement with the crucial roles played by 5-HT, many drugs target 5-HT receptors (5-HTRs). Therefore, it is unsurprising that many efforts have been devoted to discovering multitarget-directed ligands (MTDLs) capable of engaging one or more 5-HTRs plus another target phenotypically linked to a particular disease. In this review, we will describe medicinal chemistry efforts in designing MTDLs encompassing activity for one or more 5-HTRs, starting with atypical antipsychotics and moving to dual 5-HT1AR/serotonin transporter ligands, 5-HT6R antagonists/acetyl cholinesterases inhibitors, and 5-HT4R agonists/acetyl cholinesterases inhibitors. We will also provide an outlook on the most recent efforts made in the field. |
| Document Type: | article |
| File Description: | electronic resource |
| Language: | English |
| ISSN: | 1424-8247 |
| Relation: | https://www.mdpi.com/1424-8247/17/9/1238; https://doaj.org/toc/1424-8247 |
| DOI: | 10.3390/ph17091238 |
| Access URL: | https://doaj.org/article/4111d15bed8547cabd7a758ceca6537e |
| Accession Number: | edsdoj.4111d15bed8547cabd7a758ceca6537e |
| Database: | Directory of Open Access Journals |
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| ISSN: | 14248247 |
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| DOI: | 10.3390/ph17091238 |
| Published in: | Pharmaceuticals |
| Language: | English |