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.
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 . .
