Loading...
*  Histamine H2 receptor
Inhibition of neutrophil activation and chemotaxis H2-receptor antagonist GRCh38: Ensembl release 89: ENSG00000113749 - Ensembl ... Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin- ... 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 ...
*  Terfenadine
... acts as a peripherally-selective antihistamine, or antagonist of the histamine H1 receptor. It is a prodrug, ...
*  Histamine H1 receptor
Horváth BV, Szalai C, Mándi Y, László V, Radvány Z, Darvas Z, Falus A (Nov 1999). "Histamine and histamine-receptor antagonists ... 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 ... Within the brain, histamine is synthesized exclusively by neurons with their cell bodies in the tuberomammillary nucleus (TMN) ...
*  Cimetidine
Tagamet®: Discovery of Histamine H2-receptor Antagonists from American Chemical Society National Historic Chemical Landmarks. ... Cimetidine's mechanism of action as an antacid is as a histamine H2 receptor antagonist. Cimetidine is a potent inhibitor of ... 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 ...
*  Dimetotiazine
It is a serotonin antagonist and histamine antagonist. Shimazawa, M; Hara, H; Watano, T; Sukamoto, T (August 1995). "Effects of ...
*  Niperotidine
... 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 ...
*  Carbinoxamine
... is a histamine antagonist, specifically an H1-antagonist. The maleic acid salt of the levorotatory isomer is sold ...
*  Recreational drug use
... "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 (a happy sensation). Stimulants or ...
*  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- ...
*  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 ...
*  JNJ-5207852
... is a histamine antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies, ... Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in ... 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 ...
*  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
... 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 ... "Characterization of histamine H3 receptors in mouse brain using the H3 antagonist 125Iiodophenpropit". Naunyn-Schmiedeberg's ...
*  Histaminergic
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. ...
*  Loratadine
The potency of second generation histamine antagonists is (from strongest to weakest) desloratadine (Ki 0.4 nM) > ... Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H1-receptors. ...
*  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 ...
*  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. ...
*  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 ... "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 ( ...
*  Pseudoephedrine/loratadine
Loratadine is a long-acting antihistamine (H1 histamine antagonist) that is less sedating than older substances of its type. ...
*  Rupatadine
... long-acting histamine antagonist with selective peripheral H1 receptor antagonist activity. It further blocks the receptors of ... orally active dual antagonist of histamine and platelet-activating factor (PAF)". The Journal of Pharmacology and Experimental ... Rupatadine is a second generation antihistamine and PAF antagonist used to treat allergies. It was discovered and developed by ...
*  Antihistamine
Normally, histamine binds to the H1 receptor and heightens the receptor's activity; the receptor antagonists work by binding to ... Histamine receptors exhibit constitutive activity, so antihistamines can function as either a neutral receptor antagonist or an ... Histamine antagonist at the US National Library of Medicine Medical Subject Headings (MeSH) Antihistamine information at ... This history has led to contemporary research into drugs which are H3 receptor antagonist and which affect the Histamine H4 ...
*  Pressing
... , a generic drug name of Hemofarm Group for Loratadine, a second-generation H1 histamine antagonist drug used to treat ...
*  Dacemazine
... (INN, also known as Ahistan and Histantine) is a phenothiazine derivative which acts as an histamine antagonist at ...
*  Alcaftadine
... 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 in 2010 under the trade name ... This effect on histamine receptors seems to show lower rates of itching, eosinophil recruitment and redness after exposure to ...
*  General anaesthesia
... and histamine antagonists such as famotidine. Non-pharmacologic preanaesthetic interventions include playing relaxing music, ... Halothane has been found to be a GABA agonist, and ketamine is an NMDA receptor antagonist. Prior to a planned procedure, the ... Harrison, N.; Simmonds, M. (1985). "Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral ... Administration of a μ-opioid antagonist such as alvimopan immediately after surgery can help reduce the severity and duration ...
*  Nonsteroidal antiandrogen
An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. Also inhibits ... They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... Similar to enzalutamide and apalutamide, but with increased efficacy as an AR antagonist, little or no central nervous system ... Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist, improved activity against mutated AR ...
*  Clemastine
... is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of ... Effects of histamine (which are countered by antihistamines) include: Increased capillary permeability Increased capillary ... Antihistamines do not chemically inactivate or prevent the normal release of histamine. Clemastine does also act as FIASMA ( ... Antihistamines act by competitively binding to H1-receptor sites, thus blocking the binding endogenous histamine. ...