Histamine, Bradykinin, and Their Antagonists". In Brunton L (ed.). Goodman & Gilman's The Pharmacological Basis of Therapeutics ... Krystal AD, Richelson E, Roth T (August 2013). "Review of the histamine system and the clinical effects of H1 antagonists: ... Diphenhydramine, while traditionally known as an antagonist, acts primarily as an inverse agonist of the histamine H1 receptor ... "Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole". FEBS ...

... is a histamine H2 receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate ... Durant, G. J.; Emmett, J. C.; Ganellin, C. R.; Roe, A. M.; Slater, R. A. (1976). "Potential histamine H2-receptor antagonists. ... ISBN 978-0-19-850346-0. "Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. ... "Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine". Journal of ...

Fedorowicz, Zbys; van Zuuren, Esther J; Hu, Nianfang (2012-03-14). "Histamine H2-receptor antagonists for urticaria". Cochrane ... H2-receptor antagonists are sometimes used in addition to H1-antagonists to treat urticaria, but there is limited evidence for ... Histamine and other proinflammatory substances are released from mast cells in the skin and tissues in response to the binding ... Ingestion of free histamine released by bacterial decay in fish flesh may result in a rapid-onset, allergic-type symptom ...

"Clinical Development of Histamine H4 Receptor Antagonists". Histamine and Histamine Receptors in Health and Disease. Handbook ... "Clinical Development of Histamine H4 Receptor Antagonists". Histamine and Histamine Receptors in Health and Disease. Handbook ... Toreforant (JNJ-38518168) is an orally-dosed selective antagonist of the histamine H4 receptor that has been studied for ... 2018). "The Role of Histamine and Histamine Receptors in Mast Cell-Mediated Allergy and Inflammation: The Hunt for New ...

"Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. American Chemical Society. ... California Discovery of histamine H2-receptor antagonists and the introduction of Tagamet by scientists at Smith Kline and ...

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

The mechanism of action of cimetidine as an antacid is as a histamine H2 receptor antagonist. It has been found to bind to the ... Sivelle PC, Underwood AH, Jelly JA (March 1982). "The effects of histamine H2 receptor antagonists on androgen action in vivo ... Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid ... "Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. American Chemical Society. ...

Histamine, Bradykinin, and Their Antagonists Stefan Offermanns; Walter Rosenthal (2008). Encyclopedia of Molecular Pharmacology ...

... acts as a highly selective antagonist of the histamine H1 receptor. The Ki values for the H1 receptor are ... Simons FE, Simons KJ (May 1999). "Clinical pharmacology of new histamine H1 receptor antagonists". Clinical Pharmacokinetics. ... "Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models". European Journal of ... Because the symptoms of itching and redness in these conditions are caused by histamine acting on the H1 receptor, blocking ...

Bain, William Alexander (1953). "Contributions to the study of histamine antagonists in man". D.Sc. hdl:1842/26193. Mogey, ... Contributions to the study of histamine antagonists in man." The work of Bain and his department gave rise to the adrenergic- ... He measured the area of a wheal provoked by the intradermal injection of histamine before, and at various times after, an ...

"New Histamine H2-Receptor Antagonists Are on the Way". InPharma. 251 (1): 3-4. August 1980. doi:10.1007/bf03317207. ISSN 0156- ... Antihistamines target the molecule histamine by blocking the histamine H1 receptor. First-generation antihistamines like ... μ-opioid receptor antagonists are usually well-tolerated and have no abuse potential since they do not cause physical ... Phan NQ, Bernhard JD, Luger TA, Ständer S (October 2010). "Antipruritic treatment with systemic μ-opioid receptor antagonists: ...

... is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. Astemizole is rapidly ... This suppresses the formation of edema and pruritus (caused by histamine). Despite some earlier reports that astemizole does ... Astemizole may also act on histamine H3 receptors, thereby producing adverse effects.[citation needed] Astemizole does also act ... H1 receptor antagonists, HERG blocker, Janssen Pharmaceutica, Phenol ethers, Piperidines, Withdrawn drugs). ...

... 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). ...

... is an antagonist at three of the histamine receptors (1, 2 and 4). The main indication for Alcaftadine is for ... It is a H1 histamine receptor antagonist. It was approved by the U.S. Food and Drug Administration (FDA) in July 2010, under ... This effect on histamine receptors seems to show lower rates of itching, eosinophil recruitment and redness after exposure to ... H1 receptor antagonists, Mast cell stabilizers, AbbVie brands, Ophthalmology drugs). ...

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 ... "The Alkaloid Conessine and Analogues as Potent Histamine H3Receptor Antagonists". Journal of Medicinal Chemistry. 51 (17): 5423 ... "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). ...

... is an H2 histamine receptor antagonist that works by blocking histamine, thus decreasing the amount of acid released ... Ranitidine and other histamine H2 receptor antagonists may increase the risk of pneumonia in hospitalised patients. They may ... Its development was a response to the first in class histamine H2 receptor antagonist, cimetidine, developed by Sir James Black ... Force RW, Nahata MC (October 1992). "Effect of histamine H2-receptor antagonists on vitamin B12 absorption". The Annals of ...

It is a serotonin antagonist and histamine antagonist. The Sandmeyer reaction on o-(4-Dimethylaminosulfonyl-2-nitrophenylthio) ... H1 receptor antagonists, Phenothiazines, Serotonin receptor antagonists, Sulfonamides, All stub articles, Analgesic 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. ...

An H3 receptor antagonist is a type of antihistaminic drug used to block the action of histamine at H3 receptors. Unlike the H1 ... Though histamine plays a well documented role in AD, the varying levels of histamine in different areas of the brain make it ... March 2008). "Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its ... H3R antagonism leads to histamine release into the cerebrospinal fluid which promotes wakefulness. Therefore, H3R antagonists ...

... "histamine antagonists") inhibit the release or action of histamine. "Antihistamine" can be used to describe any histamine ... antagonist, but the term is usually reserved for the classical antihistamines that act upon the H1 histamine receptor. ... An allergic reaction causes release of histamine by the body. Other uses of antihistamines are to help with normal symptoms of ... histamine or acetylcholine activity. Some are also capable of inducing feelings of euphoria. The most widely used depressant by ...

... 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 ... "Histamine and Histamine Receptors in Tourette Syndrome and Other Neuropsychiatric Conditions." Neuropharmacology 106 (July 2016 ... Mouse-models and other research demonstrated that reducing histamine concentration in the H3R causes tics, but adding histamine ...

ISBN 0-444-52166-6. Lapa G, Mathews T, Harp J, Budygin E, Jones S (2005). "Diphenylpyraline, a histamine H1 receptor antagonist ... H1 receptor antagonists, Piperidines, Diphenylmethanol ethers, Stimulants, All stub articles, Respiratory system drug stubs). ...

... is a histamine antagonist, specifically an H1-antagonist. The maleic acid salt of the levorotatory isomer is sold ... H1 receptor antagonists, Chlorobenzenes, 2-Pyridyl compounds, Ethers, All stub articles, Respiratory system drug stubs). ...

1986). "Histamine antagonists and d-tubocurarine-induced hypotension in cardiac surgical patients". Clin. Pharmacol. Ther. 40 ( ... Cis-atracurium is very similar to atracurium except it is more potent and has a weaker tendency to cause histamine release. ... Histamine release is a common attribute of benzylisoquinolinium muscle relaxants. This problem generally decreases with ... That is, they bind to the receptor as antagonists and that leaves fewer receptors available for acetylcholine to bind. ...

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 ... 30 May 2022). "pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of ... by inhibiting histamine synthesis and release upon binding to endogenous histamine. By preventing the binding 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 a histamine antagonist selective for the H2 subtype. It was studied as a treatment for excessive gastric ... Palasciano, G; Maggi, V; Portincasa, P (1990). "The effect of the H2-antagonist niperotidine on intragastric acidity in healthy ... H2 receptor antagonists, Hepatotoxins, Nitroethenes, Thioethers, All stub articles, Gastrointestinal system drug stubs). ...

... 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, ...