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Histamine and its Effects Mediated via H3 Receptor – Potential Clinical Applications of H3 Antagonists [PDF]

Acta Medica Martiniana, 2013
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   +2 more sources

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

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
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Non-imidazole heterocyclic histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2003
Continued exploration of the SAR around the lead imidazopyridine histamine H(3) antagonist 1 has led to the discovery of several related series of heterocyclic histamine H(3) antagonists. The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described.
Wenying Chai, J. Guy Breitenbucher, Annette K. Kwok, Xiaobing Li, Victoria Wong, Nicholas I. Carruthers, Timothy W. Lovenberg, Curt Mazur, Sandy J. Wilson, Frank U. Axe, Todd K. Jones   +10 more
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2-Aryloxymethylmorpholine histamine H3 antagonists

Bioorganic & Medicinal Chemistry Letters, 2008
The synthesis and biological activity of a new series of 2-aryloxymethylmorpholine histamine H(3) antagonists is described. The new compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain.
Michael A. Letavic, John M. Keith, Kiev S. Ly, Pascal Bonaventure, Mark A. Feinstein, Brian Lord, Kirsten L. Miller, S. Timothy Motley, Diane Nepomuceno, Steven W. Sutton, Nicholas I. Carruthers   +10 more
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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

Histamine H3 receptor inverse agonists/antagonists influence intra-regional cortical activity and inter-regional synchronization during resting state: an exploratory cortex-wide imaging study in mice [PDF]

Molecular Brain
The histaminergic system plays a key role in modulating learning and memory, wakefulness, and energy balance. Histamine H3 receptors constitutively inhibit the synthesis and release of histamine and other neurotransmitters. Therefore, H3 receptor inverse
Sentaro Kaita, Yoshikazu Morishita, Kenta Kobayashi, Hiroshi Nomura   +3 more
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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
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Neurotransmitters and Immunity: Molecular Mechanisms, Biological Functions, Diseases, and Potential Therapeutic Targets. [PDF]

MedComm (2020)
Role of neurotransmitters in multiple pathological processes. Various neurotransmitters, including ACh, EPI, NE, 5‐HT, histamine, DA, glutamate, GABA, and neuropeptides participate in regulating key pathological events, including tumor proliferation, tumor migration, remodeling of the immune microenvironment, and the development of NDDs and ...
Li G, Li F, Tang Y, Guo S, Yao Y, Fang Y, Zhang B, Jiang Y, Wang J, Wu D, Cheng J, Huang Z, Xin Z, Zhang T.   +13 more
europepmc   +2 more sources

Anticonvulsive effect of nonimidazole histamine H3 receptor antagonists

Behavioural Pharmacology, 2014
To determine the potential of histamine H3 receptor (H3R) ligands as new antiepileptic drugs (AEDs), aromatic ether, and diether derivatives (1-12) belonging to the nonimidazole class of ligands, with high in-vitro binding affinity at human H3R, were tested for their in-vivo anticonvulsive activity in the maximal electroshock (MES)-induced and ...
Bassem Sadek, Kamil Kuder, Subramanian Dhanasekaran, Mohamed Shafiullah, Holger Stark, Dorota Łażewska, Abdu Adem, Katarzyna Kieć‐Kononowicz   +7 more
openalex   +5 more sources