Приказ основних података о документу
Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities
dc.creator | Nikolić, Katarina | |
dc.creator | Filipić, Slavica | |
dc.creator | Agbaba, Danica | |
dc.creator | Stark, Holger | |
dc.date.accessioned | 2019-09-02T11:41:27Z | |
dc.date.available | 2019-09-02T11:41:27Z | |
dc.date.issued | 2014 | |
dc.identifier.issn | 1755-5930 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/2196 | |
dc.description.abstract | The histamine H-3 receptor (H3R) is an important modulator of numerous central control mechanisms. Novel lead optimizations for H3R antagonists/inverse agonists involved studies of structure-activity relationships, cross-affinities, and pharmacokinetic properties of promising ligands. Blockade of inhibitory histamine H-3 autoreceptors reinforces histaminergic transmission, while antagonism of H-3 heteroreceptors accelerates the corticolimbic liberation of acetylcholine, norepinephrine, glutamate, dopamine, serotonin and gamma-aminobutyric acid (GABA). The H3R positioned at numerous neurotransmission crossroads indicates therapeutic applications of small-molecule H3R modulators in a number of psychiatric and neurodegenerative diseases with various clinical candidates available. Dual target drugs displaying H3R antagonism/inverse agonism with inhibition of acetylcholine esterase (AChE), histamine N-methyltransferase (HMT), or serotonin transporter (SERT) are novel class of procognitive agents. Main chemical diversities, pharmacophores, and pharmacological profiles of procognitive agents acting as H3R antagonists/inverse agonists and dual H3R antagonists/inverse agonists with inhibiting activity on AChE, HMT, or SERT are highlighted here. | en |
dc.publisher | Wiley, Hoboken | |
dc.relation | EU COST Action CM 1103 | |
dc.relation | Translational Research Innovation-Pharma (TRIP) | |
dc.relation | Fraunhofer-Projektgruppe fur Translationale Medizin und Pharmakologie (TMP) | |
dc.rights | restrictedAccess | |
dc.source | CNS Neuroscience & Therapeutics | |
dc.subject | AChE | en |
dc.subject | Histamine H-3 receptor | en |
dc.subject | HMT | en |
dc.subject | Pharmacophore | en |
dc.subject | Procognitive | en |
dc.subject | SERT | en |
dc.title | Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Николић, Катарина; Старк, Холгер; Aгбаба, Даница; Филипић, Славица; | |
dc.citation.volume | 20 | |
dc.citation.issue | 7 | |
dc.citation.spage | 613 | |
dc.citation.epage | 623 | |
dc.citation.other | 20(7): 613-623 | |
dc.citation.rank | M21 | |
dc.identifier.wos | 000337724000006 | |
dc.identifier.doi | 10.1111/cns.12279 | |
dc.identifier.pmid | 24836924 | |
dc.identifier.scopus | 2-s2.0-84902546230 | |
dc.type.version | publishedVersion |