Results 71 to 80 of about 618,319 (304)

In Silico to In Cerebro—Development of the Orexin Receptor Antagonist “Photorexant” for Photomodulation In Vitro and in Mouse Brains

open access: yesAngewandte Chemie International Edition, EarlyView.
Following a structure‐based design approach, photoswitchable derivatives of the FDA‐approved drug suvorexant were designed, docked, synthesized, and characterized pharmacologically at the orexin 1 and 2 receptors (OX1R and OX2R). Optimized “photorexant” showed up to an 11‐fold difference in IC50 between photoisomers, enabled dynamic and reversible ...
Marcus Angermann   +10 more
wiley   +1 more source

Hippocampal histamine receptors and conflictive exploration in the rat: studies using the elevated asymmetric plus-maze

open access: yesBrazilian Journal of Medical and Biological Research, 1997
The possible role of histamine receptors in the hippocampal formation on the exploratory motivation and emotionality of the rat was studied. An elevated asymmetric plus-maze composed of 4 different arms (no walls, single high wall, high and low walls and
M.B. Ruarte, A.G. Orofino, E.O. Alvarez
doaj   +1 more source

Opposite effects of mepyramine on JNJ 7777120-induced amelioration of experimentally induced asthma in mice in sensitization and provocation. [PDF]

open access: yesPLoS ONE, 2012
BACKGROUND:Histamine is detected in high concentrations in the airways during an allergic asthma response. In a murine model of allergic asthma, JNJ 7777120, an antagonist at the histamine H(4) receptor, reduces asthmatic symptoms, while the histamine H ...
Silke Beermann   +4 more
doaj   +1 more source

Ursolic Acid Alleviates Orchitis via Modulating Ferroptosis in Peritubular Myoid Cells of Testis

open access: yesAnimal Research and One Health, EarlyView.
Ursolic acid modulates key ferroptosis‐related pathways in the peritubular myoid cells of the testis in forest musk deer. ABSTRACT Chronic stress adversely affects reproductive health, increasing susceptibility to pathologies such as orchitis. Additionally, the maintenance of iron homeostasis is essential for preserving the function of the testicles ...
Yang Wang   +11 more
wiley   +1 more source

ANTI-INFLAMMATORY AND ANTI-ALLERGIC FEATURES OF ANTIBODIES TO HISTAMINE IN RELEASE-ACTIVE FORM: REVIEW OF EXPERIMENTAL AND CLINICAL RESEARCHES

open access: yesДетские инфекции (Москва), 2015
Preclinical and clinical studies of medical preparations (rengalin, ergoferon) containing release-active (P-A) antibodies to histamine confirmed their ability to provide anti-inflammatory and anti-allergic effect.
E. S. Zhavbert   +2 more
doaj   +1 more source

Gut Health in Ostriches (Struthio camelus): Insights Into Intestinal Structure, Functions, Microbiome, and Improvement Strategies

open access: yesAnimal Research and One Health, EarlyView.
Our paper systematically reviews the intestinal structure, function, and microbiota of ostriches, along with strategies for improving their gut health. We analyze how these factors collectively influence intestinal homeostasis and ostrich welfare, emphasizing probiotics as a promising intervention to enhance gut health, boost population well‐being, and
Zi‐Qun Zhang   +6 more
wiley   +1 more source

Functional characterisation of the novel histamine H(3) receptor agonist, VUF 5810, on the guinea-pig isolated ileum

open access: yes, 2003
It is known that the activation of prejunctionally-located histamine H3 receptors down-regulates the exocytotic acetylcholine release from the myenteric plexus and thus produces a negative control on the intestinal motility [1].
POZZOLI, Cristina   +7 more
core   +1 more source

Navigating adverse immunostimulation: A practical guide for clinical researchers

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Problem Setting As drug development moves towards more complex products, early clinical development programmes are increasingly hampered by unwanted and/or unexpected activation of the immune system (adverse immune stimulation, AIS). Solution At the Centre for Human Drug Research, we have introduced standardized procedures to make AIS manageable, while
Juliette A. van den Noort   +3 more
wiley   +1 more source

Clozapine:norclozapine ratio as a marker of metabolic risk and therapeutic response and effect of valproate on clozapine levels

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Aims Clozapine is the most effective antipsychotic in treatment‐resistant schizophrenia. Clozapine causes weight gain and increased diabetes risk. The role of its metabolite norclozapine and clozapine:norclozapine ratio (CLZ/NCLZ) in metabolic effects has been debated.
Susanna Maria Rask   +6 more
wiley   +1 more source

The contrast effect of blocker of AMPA/KA glutamatereceptors IEM 1751 on stimulated gastric acid secretionby pentagastrin and histamine in rats

open access: yesCurrent Issues in Pharmacy and Medical Sciences, 2009
In acute experiments on 71 white rats by the method of isolated stomach perfusion by Ghosh and Schild it was established that in rats with an intact nervous system antagonist of central and peripheral AMPA/KA glutamate receptors IEM 1751 did not ...
Tetyana Falalyeyeva   +2 more
doaj  

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