Multiple Targeting Approaches on Histamine H3 Receptor Antagonists
With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2016-05-01
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| Series: | Frontiers in Neuroscience |
| Subjects: | |
| Online Access: | http://journal.frontiersin.org/Journal/10.3389/fnins.2016.00201/full |
| _version_ | 1818515898258948096 |
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| author | Mohammad eKhanfar Anna eAffini Kiril eLutsenko Katarina eNikolic Stefania eButini Holger eStark |
| author_facet | Mohammad eKhanfar Anna eAffini Kiril eLutsenko Katarina eNikolic Stefania eButini Holger eStark |
| author_sort | Mohammad eKhanfar |
| collection | DOAJ |
| description | With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications, the combination of pharmacological properties in one molecule for improved pharmacological effects and reduced unwanted side-effects is rationally based on the increasing knowledge on the complex neurotransmitter regulations. The polypharmacological approaches on histamine H3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures. |
| first_indexed | 2024-12-11T00:34:55Z |
| format | Article |
| id | doaj.art-006655821985422687001c5025a5596c |
| institution | Directory Open Access Journal |
| issn | 1662-453X |
| language | English |
| last_indexed | 2024-12-11T00:34:55Z |
| publishDate | 2016-05-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Neuroscience |
| spelling | doaj.art-006655821985422687001c5025a5596c2022-12-22T01:27:11ZengFrontiers Media S.A.Frontiers in Neuroscience1662-453X2016-05-011010.3389/fnins.2016.00201190179Multiple Targeting Approaches on Histamine H3 Receptor AntagonistsMohammad eKhanfar0Anna eAffini1Kiril eLutsenko2Katarina eNikolic3Stefania eButini4Holger eStark5Heinrich Heine UniversityHeinrich Heine UniversityHeinrich Heine UniversityUniversity of BelgradeUniversity of SienaHeinrich Heine UniversityWith the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications, the combination of pharmacological properties in one molecule for improved pharmacological effects and reduced unwanted side-effects is rationally based on the increasing knowledge on the complex neurotransmitter regulations. The polypharmacological approaches on histamine H3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures.http://journal.frontiersin.org/Journal/10.3389/fnins.2016.00201/fullEnzymesHistaminetransporterNOGPCRMultiple targeting |
| spellingShingle | Mohammad eKhanfar Anna eAffini Kiril eLutsenko Katarina eNikolic Stefania eButini Holger eStark Multiple Targeting Approaches on Histamine H3 Receptor Antagonists Frontiers in Neuroscience Enzymes Histamine transporter NO GPCR Multiple targeting |
| title | Multiple Targeting Approaches on Histamine H3 Receptor Antagonists |
| title_full | Multiple Targeting Approaches on Histamine H3 Receptor Antagonists |
| title_fullStr | Multiple Targeting Approaches on Histamine H3 Receptor Antagonists |
| title_full_unstemmed | Multiple Targeting Approaches on Histamine H3 Receptor Antagonists |
| title_short | Multiple Targeting Approaches on Histamine H3 Receptor Antagonists |
| title_sort | multiple targeting approaches on histamine h3 receptor antagonists |
| topic | Enzymes Histamine transporter NO GPCR Multiple targeting |
| url | http://journal.frontiersin.org/Journal/10.3389/fnins.2016.00201/full |
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