Neuronal histamine and the memory of emotionally salient events

G Provensi, MB Passani, A Costa… - British journal of …, 2020 - Wiley Online Library
In this review, we describe the experimental paradigms used in preclinical studies to unravel
the histaminergic brain circuits that modulate the formation and retrieval of memories …

[HTML][HTML] Histamine beyond its effects on allergy: Potential therapeutic benefits for the treatment of Amyotrophic Lateral Sclerosis (ALS)

C Volonté, S Apolloni, M Sabatelli - Pharmacology & Therapeutics, 2019 - Elsevier
ALS currently remains a challenge despite many efforts in performing successful clinical
trials and formulating therapeutic solutions. By learning from current failures and striving for …

Development of a Conformational Histamine H3 Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists

H Schihada, X Ma, U Zabel, HF Vischer, G Schulte… - ACS …, 2020 - ACS Publications
The histamine H3 receptor (H3R) represents a highly attractive drug target for the treatment
of various central nervous system disorders, but the discovery of novel H3R targeting …

Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer's disease

D Łażewska, M Bajda, M Kaleta, P Zaręba… - European Journal of …, 2020 - Elsevier
Abstract Design and development of multitarget-directed ligands (MTDLs) has become a
very important approach in the search of new therapies for Alzheimer's disease (AD). In our …

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 …

[HTML][HTML] Multitargeting Histamine H3 Receptor Ligands among Acetyl- and Propionyl-Phenoxyalkyl Derivatives

D Łażewska, M Kaleta, P Zaręba, J Godyń, M Dubiel… - Molecules, 2023 - mdpi.com
Alzheimer's disease (AD) is a neurodegenerative disorder, for which there is no effective
cure. Current drugs only slow down the course of the disease, and, therefore, there is an …

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

DM Riddy, AE Cook, DM Shackleford, TL Pierce… - …, 2019 - Elsevier
The histamine H 3 receptor is a G protein-coupled receptor (GPCR) drug target that is highly
expressed in the CNS, where it acts as both an auto-and hetero-receptor to regulate …

Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent

K Szczepańska, S Pockes, S Podlewska… - European Journal of …, 2021 - Elsevier
A series of 4-pyridylpiperazine derivatives with varying regulatory region substituents proved
to be potent histamine H 3 receptor (H 3 R) ligands in the nanomolar concentration range …

High-Throughput Screening (HTS) Technology

A Roy - Encyclopedia of Molecular Pharmacology, 2022 - Springer
A cation current that slowly activates upon membrane hyperpolarization was detected in a
variety of excitable cells including neurons and cardiac pacemaker cells in the late 1970s …

Design, synthesis, and biological evaluation of novel oxadiazole-and thiazole-based histamine H3R ligands

MA Khanfar, D Reiner, S Hagenow, H Stark - Bioorganic & Medicinal …, 2018 - Elsevier
Abstract Histamine H 3 receptor (H 3 R) is largely expressed in the CNS and modulation of
the H 3 R function can affect histamine synthesis and liberation, and modulate the release of …