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*  Histamine H2 receptor
Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin- ... "Entrez Gene: HRH2 histamine receptor H2". Maguire JJ, Davenport AP (29 November 2016). "H2 receptor". IUPHAR/BPS Guide to ... "Histamine Receptors: H2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... The drug betazole is an example of a histamine H2 receptor agonist. Histamine is a ubiquitous messenger molecule released from ...
*  Histamine H1 receptor
"The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders". Trends in Pharmacological Sciences ... The H1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is ... Histamine H1 receptors are activated by endogenous histamine, which is released by neurons that have their cell bodies in the ... "Histamine Receptors: H1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
*  Histamine H3 receptor
1997 H3 receptors shown to modulate ischemic norepinephrine release in animals. 1999 H3 receptor cloned 2000 H3 receptors ... Leurs R, Bakker RA, Timmerman H, de Esch IJ (Feb 2005). "The histamine H3 receptor: from gene cloning to H3 receptor drugs". ... Leurs R, Bakker RA, Timmerman H, de Esch IJ (Feb 2005). "The histamine H3 receptor: from gene cloning to H3 receptor drugs". ... H3 receptors function as presynaptic autoreceptors on histamine-containing neurons. The diverse expression of H3 receptors ...
*  Imetit
... is a histamine H3 receptor agonist. Garbarg, M; Arrang, JM; Rouleau, A; Ligneau, X; Tuong, MD; Schwartz, JC; Ganellin, ... CR (1992). "S-2-(4-imidazolyl)ethylisothiourea, a highly specific and potent histamine H3 receptor agonist". The Journal of ...
*  Clobenpropit
H3 receptor antagonist Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to ... Clobenpropit is a histamine H3 receptor antagonist. It has neuroprotective effects via stimulation of GABA release in the brain ... Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z (2007). "The histamine H3 receptor antagonist clobenpropit ...
*  Immepip
... is a histamine H3 receptor agonist. Cannon KE, Leurs R, Hough LB (2007). "Activation of peripheral and spinal histamine ... H3 receptors inhibits formalin-induced inflammation and nociception, respectively". Pharmacol. Biochem. Behav. 88 (1): 122-9. ...
*  Histidine decarboxylase
There are four different histamine receptors, H1, H2, H3, and H4, each of which carries a different biological significance. H1 ... H3 controls histamine turnover by feedback inhibition of histamine synthesis and release. Finally, H4 plays roles in mast cell ... "Entrez Gene: histidine decarboxylase". Shahid, Mohammad (2009). "Histamine, Histamine Receptors, and their Role in ... "Identification of two H3-histamine receptor subtypes". Molecular Pharmacology. 38 (5): 610-613. ISSN 0026-895X. PMID 2172771. ...
*  Thioperamide
H3 receptor antagonist "IUPHAR Database , Ligand Summary , thioperamide". Schwartz, Jean-Charles. The histamine H3 receptor: ... It was used by Jean-Charles Schwartz in his early experiments regarding the H3 receptor. Thioperamide was found to be an ... leading to greater release of histamine. Its action on H3 is thought to promote wakefulness and improve memory consolidation. ... antagonist of histamine autoreceptors, which negatively regulate the release of histamine, and enhances the activity of ...
*  Proxyfan
G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor ... Protean agonism at histamine H3 receptors in vitro and in vivo. Proceedings of the National Academy of Sciences USA. 2003 Sep ... Proxyfan is a histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist ... doi:10.1124/jpet.104.078865 PMID 15821027 Arrang JM, Morisset S, Gbahou F. Constitutive activity of the histamine H3 receptor. ...
*  Pitolisant
Schlicker E, Kathmann M (2017). "Role of the Histamine H3 Receptor in the Central Nervous System". Handb Exp Pharmacol. 241: ... and colleagues after the former discovered the H3 receptor. It was the first H3 receptor inverse agonist to be tested in humans ... Schwartz JC (2011). "The histamine H3 receptor: from discovery to clinical trials with pitolisant". Br. J. Pharmacol. 163 (4): ... is a potent and selective inverse agonist of the histamine H3 receptor (Ki = 0.16 nM) which was approved for the treatment of ...
*  Burimamide
... is an antagonist at the H2 and H3 histamine receptors. It is largely inactive as an H2 antagonist at physiological ... ISBN 978-0-19-850346-0. "Tagamet®: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. ... in their intent to develop a histamine antagonist for the treatment of peptic ulcers. The discovery of burimamide ultimately ... pH, but its H3 affinity is 100x higher. It is a thiourea derivative. Burimamide was first developed by scientists at Smith, ...
*  Amitriptyline
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... and 5-HT7 receptors, the α1-adrenergic receptor, the histamine H1 and H2 receptors, and the muscarinic acetylcholine receptors ... Ghoneim OM, Legere JA, Golbraikh A, Tropsha A, Booth RG (2006). "Novel ligands for the human histamine H1 receptor: synthesis, ... histamine H1 and alpha 1-adrenergic receptors in vitro". Schizophr. Res. 37 (1): 107-22. doi:10.1016/s0920-9964(98)00146-7. ...
*  Diphenhydramine
"Cloning and functional expression of the human histamine H3 receptor". Mol. Pharmacol. 55 (6): 1101-7. PMID 10347254. Liu C, Ma ... Diphenhydramine acts primarily as an inverse agonist of the histamine H1 receptor. It is a member of the ethanolamine class of ... Ghoneim OM, Legere JA, Golbraikh A, Tropsha A, Booth RG (2006). "Novel ligands for the human histamine H1 receptor: synthesis, ... It also crosses the blood-brain barrier and inversely agonizes the H1 receptors centrally. Its effects on central H1 receptors ...
*  Chlorprothixene
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods Find ... Wander TJ, Nelson A, Okazaki H, Richelson E (1987). "Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of ... Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ...
*  Maprotiline
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Kanba S, Richelson E (1984). "Histamine H1 receptors in human brain labelled with [3H]doxepin". Brain Res. 304 (1): 1-7. doi: ... It is also a strong antagonist of the H1 receptor, a moderate antagonist of the 5-HT2 and α1-adrenergic receptors, and a weak ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (2012). "Interactions of recombinant human histamine H₁R, H₂R, H₃R, ...
*  Cipralisant
"G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor ... June 1998). "High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models". ... Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent Histamine H3 receptor ligand originally developed ... "Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor". European Journal of Pharmacology. 529 ...
*  Astemizole
... may also act on histamine H3 receptors, thereby producing adverse effects.[citation needed] Astemizole does also act ... Astemizole is rapidly absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the ... Astemizole is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. ... This suppresses the formation of edema and pruritus (caused by histamine). Despite some earlier reports that astemizole does ...
*  PF-03654746
Gemkow, M.; Davenport, A.; Harich, S.; Ellenbroek, B.; Cesura, A.; Hallett, D. (2009). "The histamine H3 receptor as a ... PF-03654746 is a potent and selective histamine H3 receptor antagonist developed by Pfizer and currently undergoing clinical ... "Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker". ... "H3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers". ...
*  H3 receptor antagonist
An H3 receptor antagonist is a classification of drugs used to block the action of histamine at the H3 receptor. Unlike the H1 ... The histamine H3 receptor (H3R) was discovered in 1983 and was one of the last receptors that were discovered using ... "The histamine H3 receptor as a therapeutic drug target for CNS disorders". Drug Discovery Today. 14 (9-10): 509-515. doi: ... "Keynote review: Histamine H3 receptor antagonists reach out for the clinic". Drug Discovery Today. 10 (23-24): 1613-1627. doi: ...
*  JNJ-5207852
PMID 16310812 Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: ... JNJ-5207852 is a histamine antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies, ... November 2004). "Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist". Br. J. Pharmacol. 143 (5 ... Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in ...
*  Iodophenpropit
"Characterization of histamine H3 receptors in mouse brain using the H3 antagonist 125Iiodophenpropit". Naunyn-Schmiedeberg's ... "Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, 125I-iodophenpropit, to ... Iodophenpropit is a histamine antagonist which binds selectively to the H3 subtype. Its 125I radiolabelled form is used for ... mapping the distribution of H3 receptors in the body. Jansen, FP; Wu, TS; Voss, HP; Steinbusch, HW; Vollinga, RC; Rademaker, B ...
*  Ciproxifan
... is an extremely potent histamine H3 inverse agonist/antagonist. The histamine H3 receptor is an inhibitory ... Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (December 2004). "The histamine H3 receptor as a novel therapeutic target ... Pillot C, Ortiz J, Héron A, Ridray S, Schwartz JC, Arrang JM (August 2002). "Ciproxifan, a histamine H3-receptor antagonist/ ... Witkin JM, Nelson DL (July 2004). "Selective histamine H3 receptor antagonists for treatment of cognitive deficiencies and ...
*  Dopamine receptor D1
The D1 receptor forms heteromers with the following receptors: dopamine D2, D3, histamine H3, μ opioid. D1-D2 D1−H3−NMDA ... Histamine H3, and N-Methyl-D-Aspartate Glutamate Receptors as Targets to Prevent Neuronal Death in Alzheimer's Disease". Mol. ... "Marked changes in signal transduction upon heteromerization of dopamine D1 and histamine H3 receptors". Br. J. Pharmacol. 157 ( ... and various serotonin receptors Many typical and atypical antipsychotics are D1 receptor antagonists in addition to D2 receptor ...
*  Penicillium waksmanii
Novel Histamine H3 Receptor Ligands Produced by Penicillium waksmanii PF1270". The Journal of Antibiotics. 60 (11): 667. doi: ...
*  Tourette syndrome
"The Magnificent Two: Histamine and the H3 Receptor as Key Modulators of Striatal Circuitry." Progress in Neuro- ... "Histamine H3 Receptor as a Potential Target for Cognitive Symptoms in Neuropsychiatric Diseases." Behavioural Brain Research ... After 2010, the central role of histamine and the H3-receptor came into focus in the pathophysiology of Tourette syndrome. Also ... "Histamine and Histamine Receptors in Tourette Syndrome and Other Neuropsychiatric Conditions." Neuropharmacology 106 (July 2016 ...
*  Hydroxyzine
... and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and ... Hydroxyzine's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action ... Orzechowski RF, Currie DS, Valancius CA (January 2005). "Comparative anticholinergic activities of 10 histamine H1 receptor ... histamine receptors: contribution of Lys(191) and Thr(194)". Molecular Pharmacology. 61 (2): 391-9. doi:10.1124/mol.61.2.391. ...
*  GSK-189,254
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves ... It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine ... Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat ... The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. British Journal of Pharmacology. 2008 ...