Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie +3 more
core +2 more sources
Novel chalcone-based fluorescent human histamine H 3 receptor ligands as pharmacological tools [PDF]
Novel fluorescent chalcone-based ligands at human histamine H(3) receptors (hH(3)R) have been designed, synthesized, and characterized. Compounds described are non-imidazole analogs of ciproxifan with a tetralone motif.
Tomasch, Miriam +3 more
core +1 more source
Calyx and dimorphic neurons of mouse Scarpa's ganglion express histamine H3 receptors
Background Histamine-related drugs are commonly used in the treatment of vertigo and related vestibular disorders. The site of action of these drugs however has not been elucidated yet.
Zucca Gianpiero +5 more
doaj +1 more source
Histamine stimulates the proliferation of small and large cholangiocytes by activation of both IP3/Ca2+ and cAMP-dependent signaling mechanisms [PDF]
Although large cholangiocytes exert their functions by activation of cyclic adenosine 3',5'-monophosphate (cAMP), Ca(2+)-dependent signaling regulates the function of small cholangiocytes. Histamine interacts with four receptors, H1-H4HRs.
Fanyin Meng +15 more
core +1 more source
Neuropharmacological targets for drug action in vestibular sensory pathways [PDF]
The use of pharmacological agents is often the preferred approach to the management of vestibular dysfunction. In the vestibular sensory pathways, the sensory neuroepithelia are thought to be influenced by a diverse number of neuroactive substances that ...
Jones, Timothy A, Lee, Choongheon
core +3 more sources
Histamine and Delirium: Current Opinion
Delirium is a very common, but refractory clinical state, notably present in intensive care and in the growing aging community. It is characterized by fluctuating disturbances in a number of key behavioral features, namely cognition, mood, attention ...
Paul L. Chazot +3 more
doaj +1 more source
Histamine H3 Receptor Antagonists Go to Clinics
Within the recent years novel lead optimisations for histamine H(3) receptor antagonists made their way from bench to bedside. Structure-activity relationships, cross-affinities and side effects as well as pharmacokinetic profiling will be discussed on selected promising compound series.
Kerstin, Sander +2 more
openaire +3 more sources
The aim of this study was to investigate the effects of histamine H1 and H3 antagonists on learning and mnemonic dysfunction in mice. Two H1 antagonists, pyrilamine and clozapine, and the prototypic H3 antagonist thioperamide were used to study the role ...
Feiyong Jia +9 more
doaj +1 more source
Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze [PDF]
The role of the histamine H3 receptor (H3R) in anxiety is controversial, due to limitations in drug selectivity and limited validity of behavioral tests used in previous studies. In the present report, we describe two experiments.
Abuhamdah, Rushdie M. +4 more
core +1 more source
Histamine is one of the most important biogenic amines and it mediates numbers of physiological processes. It is also involved in majority of inflammatory diseases via its receptors H1, H2, H3 and H4.
Hanuskova E., Plevkova J.
doaj +1 more source

