Results 11 to 20 of about 6,313 (204)

Multiple Targeting Approaches on Histamine H3 Receptor Antagonists [PDF]

Frontiers in Neuroscience, 2016
With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been
Mohammad eKhanfar, Anna eAffini, Kiril eLutsenko, Katarina eNikolic, Stefania eButini, Holger eStark   +5 more
doaj   +5 more sources

Anticonvulsant effects of isomeric nonimidazole histamine H3 receptor antagonists

Drug Design, Development and Therapy, 2016
Bassem Sadek,1 Ali Saad,1 Johannes Stephan Schwed,2,3 Lilia Weizel,2 Miriam Walter,2 Holger Stark2,3 1Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, United Arab Emirates University, Al Ain, United Arab Emirates ...
Sadek B, Saad A, Schwed JS, Weizel L, Walter M, Stark H   +5 more
doaj   +4 more sources

Restless Legs Syndrome Associated With Fexofenadine Use: A Case Report. [PDF]

Clin Case Rep
Flowchart of possible fexofenadine‐induced RLS pathophysiology. ABSTRACT Restless legs syndrome (RLS) is a neurological sensorimotor disorder characterized by an irresistible urge to move the legs, typically worsening at night and leading to sleep disturbance.
Albeshry AM.
europepmc   +2 more sources

Activity-restoring mutations in the histamine H₃ receptor increase constitutive activity and reduce structural stability. [PDF]

Protein Sci
Abstract The histamine H3 receptor (H3R) is a class A G protein‐coupled receptor (GPCR) that regulates neurotransmitter release in the central nervous system. Although structures of H3R in both inactive and active states have been elucidated, the functional roles of specific residues remain unclear.
Nakajima A, Kaneko H, Oyama K, Kuchiji M, Itakura A, Arai C, Shiroishi M.   +6 more
europepmc   +2 more sources

Pitolisant Inhibits Alcohol Drinking and Improves Withdrawal Negative Affect Through Lateral Habenula Histaminergic Signaling in Mice. [PDF]

CNS Neurosci Ther
Pitolisant, an FDA‐approved H3R antagonist, counteracts the rewarding and sedative effects of ethanol, reduces alcohol intake, and alleviates the negative affect during withdrawal. This might occur via the antagonism of presynaptic autoreceptors and heteroreceptors H3Rs in the lateral habenula, thereby activating the H2R/p‐CREB/BDNF signaling and ...
Zhao Y, Fu Y, Liu T, Yang Z, Yang Z, Chen B, Zhou L, Yang J, Chen D, Han X, Tang Y, Ye JH, Miao CY, Fu R.   +13 more
europepmc   +2 more sources

The role of the host—Neutrophil biology

Periodontology 2000, EarlyView., 2023
Abstract Neutrophilic polymorphonuclear leukocytes (neutrophils) are myeloid cells packed with lysosomal granules (hence also called granulocytes) that contain a formidable antimicrobial arsenal. They are terminally differentiated cells that play a critical role in acute and chronic inflammation, as well as in the resolution of inflammation and wound ...
Iain L. C. Chapple, Josefine Hirschfeld, Alpdogan Kantarci, Asaf Wilensky, Lior Shapira   +4 more
wiley   +1 more source

Loss of Melanopsin Photoreception and Antagonism of the Histamine H3 Receptor by Ciproxifan Inhibit Light-Induced Sleep in Mice [PDF]

, 2015
Light has direct effects on sleep and wakefulness causing arousal in diurnal animals and sleep in nocturnal animals. In the present study, we assessed the modulation of light-induced sleep by melanopsin and the histaminergic system by exposing mice to ...
Colas, Damien, Heller, H. Craig, Ikeme, Jesse, Muindi, Fanuel, Ruby, Norman F.   +4 more
core   +10 more sources

Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep–Wake Cycle Disorder

Frontiers in Pharmacology, 2022
A relationship appears to exist between dysfunction of brain histamine (HA) and various neuropsychiatric brain disorders. The possible involvement of brain HA in neuropathology has gained attention recently, and its role in many (patho)physiological ...
Mera Alhusaini, Mera Alhusaini, Nermin Eissa, Nermin Eissa, Nermin Eissa, Ali K. Saad, Ali K. Saad, Rami Beiram, Rami Beiram, Bassem Sadek, Bassem Sadek   +10 more
doaj   +1 more source

QSAR study on the histamine (H3) receptor antagonists using the genetic algorithm: Multi parameter linear regression [PDF]

Journal of the Serbian Chemical Society, 2012
A quantitative structure activity relationship (QSAR) model has been produced for predicting antagonist potency of biphenyl derivatives as human histamine (H3) receptors. The molecular structures of the compounds are numerically represented by various
Adimi Maryam, Salimi Mahmoud, Nekoei Mehdi   +2 more
doaj   +1 more source

Role of Substance P on Histamine H3 Antagonist-Induced Scratching Behavior in Mice

Journal of Pharmacological Sciences, 2006
.: The purpose of the present study was to investigate the involvement of chemical mediators, other than histamine, in the scratching behavior induced by H3 antagonists.
Maria Alejandra Hossen, Toshio Inoue, Yoshifumi Shinmei, Yoko Fujii, Takeshi Watanabe, Chiaki Kamei   +5 more
doaj   +1 more source