Effects of Betahistine on the Development of Vestibular Compensation after Unilateral Labyrinthectomy in Rats by Junya Fukuda, Kazunori Matsuda, Go Sato, Tadashi Kitahara, Momoyo Matsuoka, Takahiro Azuma, Yoshiaki Kitamura, Koichi Tomita, Noriaki Takeda

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The Potent and Selective Histamine H3 Receptor Antagonist E169 Counteracts Cognitive Deficits and Mitigates Disturbances in the PI3K/AKT/GSK-3β Signaling Pathway in MK801-Induced Amnesia in Mice by Sabna Abdalla, Nermin Eissa, Petrilla Jayaprakash, Rami Beiram, Kamil J. Kuder, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Bassem Sadek

Subjects: “…histamine H3 receptors…”
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Studies on Anticonvulsant Effects of Novel Histamine H3R Antagonists in Electrically and Chemically Induced Seizures in Rats by Alaa Alachkar, Dorota Łażewska, Gniewomir Latacz, Annika Frank, Agata Siwek, Annamaria Lubelska, Ewelina Honkisz-Orzechowska, Jadwiga Handzlik, Holger Stark, Katarzyna Kieć-Kononowicz, Bassem Sadek

Subjects: “…histamine H3 receptors…”
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Novel benzothiazole derivatives as multitargeted-directed ligands for the treatment of Alzheimer’s disease by Donia E. Hafez, Mariam Dubiel, Gabriella La Spada, Marco Catto, David Reiner-Link, Yu-Ting Syu, Mohammad Abdel-Halim, Tsong-Long Hwang, Holger Stark, Ashraf H. Abadi

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The Histamine H₄ Receptor Participates in the Neuropathic Pain-Relieving Activity of the Histamine H₃ Receptor Antagonist GSK189254 by Vittoria Borgonetti, Nicoletta Galeotti

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Simultaneous Antagonism at H3R/D2R/D3R Reduces Autism-like Self-Grooming and Aggressive Behaviors by Mitigating MAPK Activation in Mice by Nermin Eissa, Mohamed Al Awad, Shilu Deepa Thomas, Karthikkumar Venkatachalam, Petrilla Jayaprakash, Sicheng Zhong, Holger Stark, Bassem Sadek

Subjects: “…histamine H3 receptor antagonist…”
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Four step total synthesis of an H3 receptor antagonist using only tools found in a typical teaching laboratory by Smith, C, Mansfield, S, Anderson, E, Burton, J

“…In this paper, synthetic organic chemistry is taken back to basics: A four step total synthesis of a potential histamine H3 receptor antagonist is completed by A-level students in a school laboratory using only basic equipment. …”

Drug‐induced increase in lysobisphosphatidic acid reduces the cholesterol overload in Niemann–Pick type C cells and mice by Moreau, D, Vacca, F, Vossio, S, Scott, C, Colaco, A, Montoya, J, Ferguson, C, Damme, M, Moniatte, M, Parton, R, Platt, F, Gruenberg, J

“…We report that thioperamide maleate, an inverse agonist of the histamine H3 receptor HRH3, increases highly selectively the levels of lysobisphosphatidic acid, without affecting any endosomal protein or function that we tested. …”

Inhibiting the proton pump: mechanisms, benefits, harms, and questions by Aronson, J

“…New drugs for the same indications continue to emerge, including potassium-competitive acid blockers, inhibitors of transient lower esophageal sphincter relaxation, serotonergic agents/prokinetics, mucosal protectants, histamine H3 receptor agonists, anti-gastrin agents, and esophageal pain modulators. …”

Pharmacokinetics and Dose Proportionality of Betahistine in Healthy Individuals by Duaa J. Al-Tamimi, Afaq M. Ammoo, Mays E. Alani, Jaafar J. Ibraheem

“…Betahistine is an analogue of histamine, and is a weak histamine H1 receptor agonist and potent histamine H3 receptor antagonist. The recommended therapeutic dose for adults ranges from 24 to 48 mg given in doses divided throughout the day. …”
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Role of Substance P on Histamine H3 Antagonist-Induced Scratching Behavior in Mice by Maria Alejandra Hossen, Toshio Inoue, Yoshifumi Shinmei, Yoko Fujii, Takeshi Watanabe, Chiaki Kamei

“…Moreover, the fact that these histamine H3 antagonists did not induce significant increases in the histamine release from rat peritoneal mast cells suggests that the histamine H3 receptor may not be present in the peripheral cells considered in this study. …”
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The Structural Basis of DL0410, a Novel Multi-Target Candidate Drug for the Treatment of Alzheimer’s Disease by Ailin Liu, Jun Zhao, Nicholas J. Huls, Matthias Zeller, Lin Wang, Tonglei Li

“…DL0410 is a promising multi-target drug candidate for AD treatment that is not only a significant inhibitor against both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) but also an antagonist of histamine H3 receptor (H3R), and its therapeutic efficacy in treating cognitive dysfunction has been validated in a series of AD-related animal models, including scopolamine-induced mice, D-galactose-induced and Aβ-induced mice, and APP/PS1 and SAMP8 mice. …”
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Is pitolisant safe for clinical use? A retrospective pharmacovigilance study focus on the post‐marketing safety by Cheng Jiang, Jiancheng Qian, Xin Jiang, Shuohan Zhang, Junxian Zheng, Hongwei Wang

“…Abstract Pitolisant, a novel histamine H3‐receptor antagonist, holds significant promise for treating narcolepsy. …”
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Effect of the Fexofenadine on the expression of HRH-1 and HRH-4 receptor in Peripheral Blood Mononuclear Cell isolated from children with diagnosed allergy – in vitro study Short c... by Natalia Kordulewska, Anna Cieślińska, Ewa Fiedorowicz, Beata Jarmołowska, Elżbieta Kostyra

“…The pleiotropic effects of histamine are mediated by four types of receptors that belong to the G-protein-coupled receptor family: histamine H1 receptor (HRH-1), histamine H2 receptor, histamine H3 receptor, and histamine H4 receptor. Our hypothesis is that HRH-4 opens new possibility in treatment in allergy diseases and FXF could be the antagonist of both HRH-1 and HRH-4. …”
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Effects of Adjunctive Betahistine Therapy on Lipid Metabolism in Patients with Chronic Schizophrenia: A Randomized Double-Blind Placebo-Controlled Study by Bai L, Liang W, Wang Y, Fan N, zhang Q, Bian Y, Yang F

“…Thus, it provides new ideas for the treatment of metabolic syndrome in patients with chronic schizophrenia.Keywords: schizophrenia, lipid metabolism, betahistine, histamine, H3-receptor antagonist…”
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Structures 4-n-propyl Piperazines as Non-Imidazole Histamine H3 Antagonists by Andrzej Olczak, Jarosław Sukiennik, Beata Olszewska, Monika Stefaniak, Krzysztof Walczyński, Małgorzata Szczesio

“…This work is a continuation of the research searching for a new lead of non-imidazole histamine H3 receptor antagonists.…”
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The Dual-Active Histamine H₃ Receptor Antagonist and Acetylcholine Esterase Inhibitor E100 Alleviates Autistic-Like Behaviors and Oxidative Stress in Valproic Acid Induc... by Nermin Eissa, Sheikh Azimullah, Petrilla Jayaprakash, Richard L. Jayaraj, David Reiner, Shreesh K. Ojha, Rami Beiram, Holger Stark, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Bassem Sadek

“…The histamine H3 receptor (H3R) functions as auto- and hetero-receptors, regulating the release of brain histamine (HA) and acetylcholine (ACh), respectively. …”
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Hypothesis: Amelioration of obesity‐induced cognitive dysfunction via a lorcaserin–betahistine combination treatment by Ike C. dela Peña, Johnny D. Figueroa, Wei‐Xing Shi

“…Given this background, we hypothesize that concomitant activation of serotonin 5‐HT2C and histamine H1 receptors, coupled with antagonism of histamine H3 receptors, synergistically modulates mesocortical dopamine neurotransmission and ameliorates obesity‐induced cognitive dysfunction. …”
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SNAP25 differentially contributes to Gi/o-coupled receptor function at glutamatergic synapses in the nucleus accumbens by Kevin M. Manz, José C. Zepeda, Zack Zurawski, Heidi E. Hamm, Brad A. Grueter, Brad A. Grueter, Brad A. Grueter, Brad A. Grueter

“…While κ opioid, CB1, adenosine A1, group II metabotropic glutamate receptors, and histamine H3 receptors inhibit glutamatergic transmission onto MSNs independent of SNAP25, we report that SNAP25 contributes significantly to the actions of GABAB, 5-HT1B/D, and μ opioid receptors. …”
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2-pentadecyl-2-oxazoline prevents cognitive and social behaviour impairments in the Amyloid β-induced Alzheimer-like mice model: Bring the α2 adrenergic receptor back into play by R. Infantino, S. Boccella, D. Scuteri, M. Perrone, F. Ricciardi, R.M. Vitale, R. Bonsale, A. Parente, I. Allocca, A. Virtuoso, C. De Luca, C. Belardo, P. Amodeo, V. Gentile, G. Cirillo, G. Bagetta, L. Luongo, S. Maione, F. Guida

“…We have previously shown that PEA-OXA behaves as an α2 adrenergic receptor (α2AR) antagonist and a putative protean agonist on histamine H3 receptors. Recently, neuroinflammation and monoaminergic neurotransmission dysfunction has drawn particular attention in Alzheimer Disease (AD) pathophysiology. …”
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