Histaminergic regulation of food intake

A Khouma, MM Moeini, J Plamondon… - Frontiers in …, 2023 - frontiersin.org
Histamine is a biogenic amine that acts as a neuromodulator within the brain. In the
hypothalamus, histaminergic signaling contributes to the regulation of numerous …

Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma-1 Receptor Antagonists with Promising Antinociceptive …

K Szczepańska, S Podlewska, M Dichiara… - ACS chemical …, 2021 - ACS Publications
In an attempt to extend recent studies showing that some clinically evaluated histamine H3
receptor (H3R) antagonists possess nanomolar affinity at sigma-1 receptors (σ1R), we …

Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain

K Szczepańska, T Karcz, M Dichiara… - Journal of Medicinal …, 2023 - ACS Publications
In search of new dual-acting histamine H3/sigma-1 receptor ligands, we designed a series
of compounds structurally based on highly active in vivo ligands previously studied and …

Histamine H3 receptor antagonists with peptidomimetic (keto) piperazine structures to inhibit Aβ oligomerisation

M Falkenstein, D Reiner-Link, A Zivkovic… - Bioorganic & medicinal …, 2021 - Elsevier
Alzheimeŕs disease (AD) is the most prominent neurodegenerative disorder with high
medical need. Protein-protein-interactions (PPI) interactions have a critical role in AD where …

KSK-74: Dual Histamine H3 and Sigma-2 Receptor Ligand with Anti-Obesity Potential

K Mika, M Szafarz, M Zadrożna, B Nowak… - International Journal of …, 2022 - mdpi.com
Many studies involving compounds that enhance histamine release, such as histamine H3
receptor (H3R) antagonists, have shown efficacy in inhibiting weight gain, but none have …

Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents–Design, synthesis, structural studies and pharmacological profiling

P Stępnicki, KM Targowska-Duda, AL Martínez… - European Journal of …, 2023 - Elsevier
Schizophrenia is a mental disorder with a complex pathomechanism involving many
neurotransmitter systems. Among the currently used antipsychotics, classical drugs acting as …

Improvement of Metabolic and Histological Changes of Adiposity in Rats by Synthetic Oleoyl Chalcones

AAM AlKhathami, HA Saad, FA Fareed… - Chemistry & …, 2023 - Wiley Online Library
We previously reported that synthetic oleoyl chalcones had a favorable effect to alleviate
metabolic consequences of obesity in male SD rats. In this work, we prepared and …

Effects of GPR18 ligands on body weight and metabolic parameters in a female rat model of excessive eating

M Kotańska, K Mika, M Szafarz, M Kubacka, CE Müller… - Pharmaceuticals, 2021 - mdpi.com
GPR18 has been proposed to play a role in the progression of metabolic disease and
obesity. Therefore, the aim of this study was to determine the effects of selective GRP18 …

The Effect of KSK-94, a Dual Histamine H3 and Sigma-2 Receptor Ligand, on Adipose Tissue in a Rat Model of Developing Obesity

M Kotańska, M Zadrożna, M Kubacka, K Mika… - Pharmaceuticals, 2024 - mdpi.com
Background: Numerous studies highlight the critical role that neural histamine plays in
feeding behavior, which is controlled by central histamine H3 and H1 receptors. This is the …

[HTML][HTML] Metabolic benefits of novel histamine H3 receptor ligands in the model of excessive eating: The importance of intrinsic activity and pharmacokinetic properties

K Mika, M Szafarz, M Bednarski, K Kuder… - Biomedicine & …, 2021 - Elsevier
Aims One of the therapeutic approaches in the treatment of obesity is the use of histamine H
3 receptor ligands. Histamine plays a significant role in eating behavior because it causes a …