In contrast, histamine H3 receptor antagonists increase wakefulness. Similar to the sedative effect of first-generation H1 ... Histamine intolerance Histamine receptor antagonist Scombroid food poisoning Photic sneeze reflex Histamine Material Safety ... The tele tautomer, Nτ-H-histamine, is preferred in solution as compared to the pros tautomer, Nπ-H-histamine. Histamine has two ... The H2 and H3 receptors are thought to be helpful when treating MS patients. Histamine has been shown to help with T-cell ...

... is a histamine H3 receptor antagonist. It has neuroprotective effects via stimulation of GABA release in brain ... Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z (2007). "The histamine H3 receptor antagonist clobenpropit ... Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in ... H3 receptor antagonists, Imidazoles, Chloroarenes, All stub articles, Nervous system drug stubs). ...

H3 receptor antagonist "Thioperamide". IUPHAR/BPS Guide to Pharmacology. Schwartz JC (June 2011). "The histamine H3 receptor: ... Thioperamide was found to be an antagonist of histamine autoreceptors, which negatively regulate the release of histamine. The ... Thioperamide is a potent HRH4 antagonist and selective HRH3 antagonist capable of crossing the blood-brain barrier. It was used ... H3 receptor antagonists, Thioureas, Piperidines, Imidazoles, Cyclohexyl compounds, All stub articles, Nervous system drug stubs ...

An H3 receptor antagonist is a type of antihistaminic drug used to block the action of histamine at H3 receptors. Unlike the H1 ... 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: ... Consequently, unlike the H1 antagonist antihistamines which are sedating, H3 antagonists have stimulant and nootropic effects, ...

... histamine receptor antagonists H3-receptor antagonist Histamine H1-receptor Histamine H2-receptor Histamine H4-receptor GRCh38 ... 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". ...

von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Dopamine antagonists, H1 receptor antagonists, Muscarinic antagonists, Serotonin receptor antagonists, Sigma agonists, Sodium ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (February 2012). "Interactions of recombinant human histamine H1, H2 ... Ghoneim OM, Legere JA, Golbraikh A, Tropsha A, Booth RG (2006). "Novel ligands for the human histamine H1 receptor: synthesis, ...

It is a histamine 3 (H3) receptor antagonist/inverse agonist. It represents the first commercially available medication in its ... Pitolisant is an inverse agonist of the histamine 3 (H3) autoreceptor. The H3 autoreceptors regulate histaminergic activity in ... By preventing the binding of endogenous histamine at the H3, as well as producing a response opposite to that of endogenous ... West RE, Zweig A, Shih NY, Siegel MI, Egan RW, Clark MA (November 1990). "Identification of two H3-histamine receptor subtypes ...

von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... D1 antagonists, D2 antagonists, D3 antagonists, D4 antagonists, D5 antagonists, H1 receptor antagonists, Muscarinic antagonists ... 5-HT2A antagonists, 5-HT6 antagonists, 5-HT7 antagonists, Alpha-1 blockers, Dimethylamino compounds, Antihistamines, ... Chlorprothixene is an antagonist of the following receptors: 5-HT2, 5-HT6, 5-HT7: antipsychotic effects, sedation/anxiolysis, ...

... 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. ...

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 ... H1 receptor antagonists, Muscarinic antagonists, Norepinephrine reuptake inhibitors, Secondary amines, Serotonin receptor ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (2012). "Interactions of recombinant human histamine H1R, H2R, H3R, ...

von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (January 2009). "Potential utility of histamine H3 receptor antagonist ... Chlorpromazine is an antagonist of several insect monoamine receptors. It is the most active antagonist known of silk moth ( ... Its mechanism of action is not entirely clear but believed to be related to its ability as a dopamine antagonist. It also has ... Histamine receptors (H1 receptors, accounting for sedation, antiemetic effect, vertigo, and weight gain) α1- and α2-adrenergic ...

"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). " ... H3 receptor antagonists, Imidazoles, All stub articles, Pharmacology stubs). ... Van Der Goot, H; Timmerman, H (2000). "Selective ligands as tools to study histamine receptors". European Journal of Medicinal ...

... is an antagonist at the H2 and H3 histamine receptors. At physiological pH, it is largely inactive as an H2 ... H2 receptor antagonists, H3 receptor antagonists, Imidazoles, Thioureas, All stub articles, Gastrointestinal system drug stubs) ... 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 ...

... is a histamine antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies, ... Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: an attractive ... 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 ...

... 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- ... H3 receptor antagonists, Imidazoles, Ureas, All stub articles, Organic compound stubs, Pharmacology stubs). ...

Subdivisions of histamine antagonists include H1 receptor antagonists, H2 receptor antagonists, and H3 receptor antagonists. ... Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). ... Histaminergic means "working on the histamine system", and histaminic means "related to histamine". A histaminergic agent (or ... drug) is a chemical which functions to directly modulate the histamine system in the body or brain. ...

Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells. BMC Pharmacology. 2008 ... to antagonist, to inverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 ... 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 ...

A-349,821 is a potent and selective histamine H3 receptor antagonist (or possibly an inverse agonist). It has nootropic effects ... April 2003). "Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists". ... a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology. 68 (5): 933-45. doi:10.1016/j.bcp. ... H3 receptor antagonist Faghih R, Dwight W, Pan JB, Fox GB, Krueger KM, Esbenshade TA, et al. ( ...

... 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 ... H3 receptor antagonists, Piperazines, Cyclopentanes, All stub articles, Gastrointestinal system drug stubs, Ketone stubs). ... "Increase of neuronal histamine in obese rats is associated with decreases in body weight and plasma triglycerides". Obesity ( ...

"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 has been used ... "Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, 125I-iodophenpropit, to ... H3 receptor antagonists, Imidazoles, Iodoarenes, All stub articles, Pharmacology stubs). ...

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 ... a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology. 68 (5): 933-45. doi:10.1016/j.bcp. ... Normally, histamine binds to the H1 receptor and heightens the receptor's activity; the receptor antagonists work by binding to ...

... is a potent and selective histamine antagonist which binds selectively to the H3 subtype. However while VUF-5681 ... Baker JG (June 2008). "Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells". ... H3 receptor antagonists, Imidazoles, 4-Piperidinyl compounds, All stub articles, Pharmacology stubs). ... "Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway". ...

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 ...

Antagonizing H3 increases histaminergic tone. Histamine antagonist Histamine+agonist at the U.S. National Library of Medicine ... H3: Betahistine is a weak Histamine1 agonist and a very strong antagonist of the Histamine3 autoreceptor. ... A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes. H2: ... Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine. ...

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 ( ... H3 receptor antagonists, Steroidal alkaloids, All stub articles, Pharmacology stubs). ... "The Alkaloid Conessine and Analogues as Potent Histamine H3Receptor Antagonists". Journal of Medicinal Chemistry. 51 (17): 5423 ...

Pitolisant, a selective histamine 3 (H3) receptor antagonist/inverse agonist, was approved by FDA during August 2019. It works ... IH has also been associated with a malfunction of the norepinephrine system and decreased cerebrospinal fluid (CSF) histamine ... Flumazenil, a GABAA receptor antagonist is approved by the FDA for use in anesthesia reversal and benzodiazepine overdose. ... Suvorexant, a hypocretin receptor antagonist, has been developed to limit the natural effects of hypocretin in patients with ...

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 ... H3 receptor antagonists, Benzonitriles, 4-Hydroxybiphenyl ethers, Pyrrolidines, Nitriles, All stub articles, Gastrointestinal ...

"Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, ... "Role of the Histamine H3 Receptor in the Central Nervous System". Histamine and Histamine Receptors in Health and Disease. ... Harwell, Victoria; Fasinu, Pius (1 September 2020). "Pitolisant and Other Histamine-3 Receptor Antagonists-An Update on ... and H3 receptor antagonist pitolisant. Some medications like widely used sociability-related GABA receptor agonist phenibut can ...

He is co-inventor of pitolisant, the first histamine H3-receptor antagonist/inverse agonist Wakix, for treating narcolepsy. ... "Charon Robin Ganellin", EHRS Tagamet: Discovery of Histamine H2-receptor Antagonists from American Chemical Society National ... 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 ...

Stark is a co-inventor of the active ingredient Pitolisant, the only histamine H3 receptor antagonist approved to date. Holger ... He is also a member of the German Chemical Society (GdCh), the European Histamine Research Society (EHRS) and the Frankfurt ... His research focuses on the development of new, synthetic receptor ligands for G protein-coupled receptors, mainly histamine ...