Results 11 to 20 of about 3,102 (198)

Homologs of Histamine as Histamine H3 Receptor Antagonists: A New Potent and Selective H3 Antagonist, 4(5)-(5-Aminopentyl)-1H-imidazole

Journal of Medicinal Chemistry, 1995
The influence of alkyl chain length variation on the histamine H3 receptor activity of histamine homologs 1 was investigated. A series of 4(5)-(omega-aminoalkyl)-1H-imidazoles 1 was prepared with an alkyl chain length varying from one methylene group to 10 methylene groups.
Roeland C. Vollinga, Wiro M. P. B. Menge, Rob Leurs, H. Timmerman   +3 more
openalex   +3 more sources

The Histamine H3 Receptor Antagonist E159 Reverses Memory Deficits Induced by Dizocilpine in Passive Avoidance and Novel Object Recognition Paradigm in Rats [PDF]

Frontiers in Pharmacology, 2017
The involvement of histamine H3 receptors (H3Rs) in memory is well known, and the potential of H3R antagonists in therapeutic management of neuropsychiatric diseases, e.g., Alzheimer disease (AD) is well established.
Alaa Alachkar, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Bassem Sadek   +3 more
doaj   +2 more sources

Efficacy and Safety of Histamine H3 Receptor Antagonist/Inverse Agonist Including Betahistine for Schizophrenia: A Systematic Review and Meta‐Analysis [PDF]

Neuropsychopharmacology Reports
Aim Whether histamine H3 receptor antagonists (H3R‐ANTs)/inverse agonists (H3R‐IAs) provides benefit for the treatment of schizophrenia remains unclear. This meta‐analysis was conducted to address the above clinical question.
Yasufumi Nishii, Kenji Sakuma, Shun Hamanaka, Nakao Iwata, Taro Kishi   +4 more
doaj   +2 more sources

Targeting Microglia in Neuroinflammation: H3 Receptor Antagonists as a Novel Therapeutic Approach for Alzheimer’s Disease, Parkinson’s Disease, and Autism Spectrum Disorder [PDF]

Pharmaceuticals
Histamine performs dual roles as an immune regulator and a neurotransmitter in the mammalian brain. The histaminergic system plays a vital role in the regulation of wakefulness, cognition, neuroinflammation, and neurogenesis that are substantially ...
Shilu Deepa Thomas, Sabna Abdalla, Nermin Eissa, Amal Akour, Niraj Kumar Jha, Shreesh Ojha, Bassem Sadek   +6 more
doaj   +2 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

Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-
Emily M. Stocking, Leah Aluisio, John Atack, Pascal Bonaventure, Nicholas I. Carruthers, Christine Dugovic, Anita Everson, Ian Fraser, Xiaohui Jiang, Perry Leung, Brian Lord, Kiev S. Ly, Kirsten L. Morton, Diane Nepomuceno, Chandravadan R. Shah, Jonathan Shelton, Akinola Soyode-Johnson, Michael A. Letavic   +17 more
openalex   +3 more sources

Alleviation of Autophagic Deficits and Neuroinflammation by Histamine H3 Receptor Antagonist E159 Ameliorates Autism-Related Behaviors in BTBR Mice [PDF]

Pharmaceuticals
Background/Objectives: Autism spectrum disorder (ASD) is a neurodevelopmental condition marked by social interaction difficulties, repetitive behaviors, and immune dysregulation with elevated pro-inflammatory markers.
Shilu Deepa Thomas, Petrilla Jayaprakash, Nurfirzana Z. H. J. Marwan, Ezzatul A. B. A. Aziz, Kamil Kuder, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Bassem Sadek   +7 more
doaj   +2 more sources

Generation and Characterization of Novel Contilisant+Tubastatin a Multitarget Small Molecules Against Glioblastoma [PDF]

Pharmaceutics
Background/Objectives: Glioblastoma is the most common and aggressive primary brain tumor in adults, with patient prognosis remaining poor. Treatment resistance and tumor recurrence are frequent, primarily due to the high intra- and inter-tumoral ...
Irati de Goñi, Aizpea Artetxe-Zurutuza, Joseba Elizazu, Raul Garcia-Garcia de Garayo, Jhonatan Vergara-Arce, Mikel Azkargorta, Mireia Toledano-Pinedo, Alicia Porro-Pérez, Felix Elortza, Jose Luis Marco-Contelles, Nicolas Sampron, Nerea Iturrioz-Rodriguez, Ander Matheu   +12 more
doaj   +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

Histamine H3 Receptor Antagonist, Thioperamide, Improves Behavioral and Neuropathological Changes Associated with Subclinical Hypersensitivity to a Cow's Milk Allergen. [PDF]

J Neuroimmune Pharmacol
Germundson-Hermanson D, Klug MG, Nagamoto-Combs K.   +2 more
europepmc   +3 more sources