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Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities

Authorized Users Only
2014
Authors
Nikolić, Katarina
Filipić, Slavica
Agbaba, Danica
Stark, Holger
Article (Published version)
Metadata
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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 a...gents. 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.

Keywords:
AChE / Histamine H-3 receptor / HMT / Pharmacophore / Procognitive / SERT
Source:
CNS Neuroscience & Therapeutics, 2014, 20, 7, 613-623
Publisher:
  • Wiley, Hoboken
Funding / projects:
  • EU COST Action CM 1103
  • Translational Research Innovation-Pharma (TRIP)
  • Fraunhofer-Projektgruppe fur Translationale Medizin und Pharmakologie (TMP)

DOI: 10.1111/cns.12279

ISSN: 1755-5930

PubMed: 24836924

WoS: 000337724000006

Scopus: 2-s2.0-84902546230
[ Google Scholar ]
29
24
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2196
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Nikolić, Katarina
AU  - Filipić, Slavica
AU  - Agbaba, Danica
AU  - Stark, Holger
PY  - 2014
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2196
AB  - 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.
PB  - Wiley, Hoboken
T2  - CNS Neuroscience & Therapeutics
T1  - Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities
VL  - 20
IS  - 7
SP  - 613
EP  - 623
DO  - 10.1111/cns.12279
ER  - 
@article{
author = "Nikolić, Katarina and Filipić, Slavica and Agbaba, Danica and Stark, Holger",
year = "2014",
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.",
publisher = "Wiley, Hoboken",
journal = "CNS Neuroscience & Therapeutics",
title = "Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities",
volume = "20",
number = "7",
pages = "613-623",
doi = "10.1111/cns.12279"
}
Nikolić, K., Filipić, S., Agbaba, D.,& Stark, H.. (2014). Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities. in CNS Neuroscience & Therapeutics
Wiley, Hoboken., 20(7), 613-623.
https://doi.org/10.1111/cns.12279
Nikolić K, Filipić S, Agbaba D, Stark H. Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities. in CNS Neuroscience & Therapeutics. 2014;20(7):613-623.
doi:10.1111/cns.12279 .
Nikolić, Katarina, Filipić, Slavica, Agbaba, Danica, Stark, Holger, "Procognitive Properties of Drugs with Single and Multitargeting H-3 Receptor Antagonist Activities" in CNS Neuroscience & Therapeutics, 20, no. 7 (2014):613-623,
https://doi.org/10.1111/cns.12279 . .

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