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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- ... Inhibition of neutrophil activation and chemotaxis H2-receptor antagonist GRCh38: Ensembl release 89: ENSG00000113749 - Ensembl ... The drug betazole is an example of a histamine H2 receptor agonist. Histamine is a ubiquitous messenger molecule released from ... Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253-78. PMID 9311023. "Entrez Gene: HRH2 histamine ...
*  Histamine H1 receptor
Horváth BV, Szalai C, Mándi Y, László V, Radvány Z, Darvas Z, Falus A (Nov 1999). "Histamine and histamine-receptor antagonists ... "The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders". Trends in Pharmacological Sciences ... Histamine H1 receptors are activated by endogenous histamine, which is released by neurons that have their cell bodies in the ... While the best characterized function of the histamine system in the brain is regulation of sleep and arousal, histamine is ...
*  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 ...
*  Amitriptyline
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Amitriptyline additionally acts as an antagonist or inverse agonist of the serotonin 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 ... It has also been shown to be a relatively weak NMDA receptor antagonist via the dizocilpine (MK-801)/phencyclidine (PCP) site. ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (2012). "Interactions of recombinant human histamine H₁R, H₂R, H₃R, ...
*  Chlorprothixene
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Chlorprothixene is an antagonist of the following receptors: 5-HT2: antipsychotic effects, anxiolysis, weight gain D1, D2, D3: ...
*  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 ... "Keynote review: Histamine H3 receptor antagonists reach out for the clinic". Drug Discovery Today. 10 (23-24): 1613-1627. doi: ... March 2008). "Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its ... Vohora, Divya; Bhowmik, Malay (2012). "Histamine H3 receptor antagonists/inverse agonists on cognitive and motor processes: ...
*  ABT-239
Potent and selective histamine H3 receptor antagonist with drug-like properties". J. Pharmacol. Exp. Ther. 313 (1): 165-75. doi ... analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists". Biochemical pharmacology. 71 (8): 1103-13. ... and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist". J. ... but is still widely used in animal research into H3 antagonists / inverse agonists. Esbenshade TA, Fox GB, Krueger KM, Miller ...
*  Maprotiline
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... 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, ... Maprotiline has also more recently been identified as a potent antagonist of the 5-HT7 receptor, with this action potentially ...
*  Cipralisant
June 1998). "High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models". ... An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute ... Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent Histamine H3 receptor ligand originally developed ... Cipralisant was initially classified as a selective H3 antagonist, but newer research (2005) suggests also agonist properties, ...
*  Ciproxifan
... is an extremely potent histamine H3 inverse agonist/antagonist. The histamine H3 receptor is an inhibitory ... 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 ... a potent histamine H3-receptor antagonist". J. Pharmacol. Exp. Ther. 287 (2): 658-66. PMID 9808693. ...
*  A-349,821
... is a potent and selective histamine H3 receptor antagonist (or possibly an inverse agonist). It has nootropic effects ... novel and selective histamine H3 receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 13 (7): 1325-8. doi:10.1016/ ... a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology. 68 (5): 933-945. doi:10.1016/j.bcp. ... "Detection of multiple H3 receptor affinity states utilizing 3HA-349821, a novel, selective, non-imidazole histamine H3 receptor ...
*  Antihistamine
This history has led to contemporary research into drugs which are H3 receptor antagonist and which affect the Histamine H4 ... An H3-antihistamine is a classification of drugs used to inhibit the action of histamine at the H3 receptor. H3 receptors are ... March 2008). "Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its ... a potent histamine H3-receptor antagonist". The Journal of Pharmacology and Experimental Therapeutics. 287 (2): 658-66. PMID ...
*  NNC 38-1049
... is a histamine antagonist selective for the H3 subtype. It has anorectic effects in animal studies and is being ... December 2005). "Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and ... Increase of neuronal histamine in obese rats is associated with decreases in body weight and plasma triglycerides. Obesity ( ...
*  Iodophenpropit
"Characterization of histamine H3 receptors in mouse brain using the H3 antagonist 125Iiodophenpropit". Naunyn-Schmiedeberg's ... Iodophenpropit is a histamine antagonist which binds selectively to the H3 subtype. Its 125I radiolabelled form is used for ... "Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, 125I-iodophenpropit, to ... mapping the distribution of H3 receptors in the body. Jansen, FP; Wu, TS; Voss, HP; Steinbusch, HW; Vollinga, RC; Rademaker, B ...
*  Impentamine
"Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H- ... Impentamine is a histamine antagonist selective for the H3 subtype. Vollinga, RC; Menge, WM; Leurs, R; Timmerman, H (1995). " ... Van Der Goot, H; Timmerman, H (2000). "Selective ligands as tools to study histamine receptors". European journal of medicinal ...
*  C. Robin Ganellin
He is co-inventor of pitolisant, the first histamine H3-receptor antagonist/inverse agonist WakixTM, for treating narcolepsy. ... 1, 2001, 13-vii-13-viii "Charon Robin Ganellin", EHRS Tagamet®: Discovery of Histamine H2-receptor Antagonists from American ... collaborating with Sir James Black researching histamine H2-receptor antagonists. This research eventually led to the discovery ... This discovery was crucial to their research, providing the impetus to search for a suitable H2-receptor antagonist to affect ...
*  JNJ-5207852
... is a histamine antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies, ... PMID 16310812 Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: ... 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 ...
*  SCH-79687
... is a histamine antagonist selective for the H3 subtype. McLeod RL, Rizzo CA, West RE Jr, Aslanian R, McCormick K, ... Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4- ...
*  GSK-189,254
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves ... Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat ... Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and ... It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine ...
*  Histamine H3 receptor
2002 H3(-/-) mice (mice that do not have this receptor) Histamine antagonist#H3-receptor antagonists GRCh38: Ensembl release 89 ... Esbenshade TA, Fox GB, Cowart MD (Apr 2006). "Histamine H3 receptor antagonists: preclinical promise for treating obesity and ... 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". ...
*  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, ...
*  Betahistine
... is a strong antagonist of the histamine H3 receptor and a weak agonist of the histamine H1 receptor. Betahistine ... The study authors suggest that hypersensitivity reactions may be a direct result of betahistine's role in increasing histamine ... More importantly, betahistine has a powerful antagonistic effects at H3 receptors, thereby increasing the levels of ... Its chemical structure closely resembles those of phenethylamine and histamine.[citation needed] Betahistine is marketed under ...
*  A-423,579
... is one of a range of histamine antagonists developed by Abbott Laboratories which are selective for the H3 subtype, ... "Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy". ... radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists". Basic ...
*  Conessine
It acts as a histamine antagonist, selective for the H3 subtype (with an affinity of pKi = 8.27; Ki = ~5 nM). It was also found ... "A new family of H3 receptor antagonists based on the natural product Conessine". Bioorganic & Medicinal Chemistry Letters. 18 ( ... "The Alkaloid Conessine and Analogues as Potent Histamine H3Receptor Antagonists". Journal of Medicinal Chemistry. 51 (17): 5423 ...
*  VUF-5681
... is a potent and selective histamine antagonist which binds selectively to the H3 subtype. However while VUF-5681 ... PMID 16769092 Baker, JG (2008). "Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in ... Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway. ... blocks the activity of more potent H3 agonists, recent studies suggest that it may have some weak partial agonist activity when ...
*  Hydroxyzine
Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (2005). "Evaluation of histamine H1-, H2-, and H3-receptor ligands ... a potent antagonist of the human histamine H(1) receptor". Eur. J. Pharmacol. 449 (3): 229-37. doi:10.1016/s0014-2999(02)02049- ... "Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models". European Journal of ... Tashiro M, Kato M, Miyake M, Watanuki S, Funaki Y, Ishikawa Y, Iwata R, Yanai K (2009). "Dose dependency of brain histamine H(1 ...
*  PF-03654746
... is a potent and selective histamine H3 receptor antagonist developed by Pfizer and currently undergoing clinical ... Gemkow, M.; Davenport, A.; Harich, S.; Ellenbroek, B.; Cesura, A.; Hallett, D. (2009). "The histamine H3 receptor as a ... "Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker". ... "The Effects of an H3 Receptor Antagonist in a Nasal Allergen Challenge Model". Journal of Allergy and Clinical Immunology. 125 ...