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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 ... Brew OB, Sullivan MH (Sep 2001). "Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto- ... The drug betazole is an example of a histamine H2 receptor agonist. Histamine is a ubiquitous messenger molecule released from ...
*  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 ... they are more properly described as H1-antihistamines rather than H1-receptor antagonists.15 Passani MB, Lin JS, Hancock A, ... The H1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is ...
*  Clemastine
... is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of ... Antihistamines act by competitively binding to H1-receptor sites, thus blocking the binding endogenous histamine. ... 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 ( ...
*  Mequitazine
"Oxidation of Histamine H1 Antagonist Mequitazine is Catalyzed by Cytochrome P450 2D6 in Human Liver Microsomes" (PDF). The ... Mequitazine (trade name Primalan) is an H1 antagonist and anticholinergic of the phenothiazine chemical class. It is used to ...
*  Astemizole
... is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. Astemizole is rapidly ... absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, ... 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 ...
*  Diphenylmethanol
It is used in the synthesis of Modafinil and the Benzhydryl group is present in the structure of many histamine H1 antagonists ...
*  Cetirizine
... acts as a highly selective antagonist of the histamine H1 receptor. The Ki values for the H1 receptor are ... It acts as a selective antagonist of the histamine H1 receptor. Second-generation antihistamines like cetirizine are less able ... Simons FE, Simons KJ (1999). "Clinical pharmacology of new histamine H1 receptor antagonists". Clin Pharmacokinet. 36 (5): 329- ... Orzechowski RF, Currie DS, Valancius CA (2005). "Comparative anticholinergic activities of 10 histamine H1 receptor antagonists ...
*  Diphenylpyraline
ISBN 0-444-52166-6. Lapa G, Mathews T, Harp J, Budygin E, Jones S (2005). "Diphenylpyraline, a histamine H1 receptor antagonist ...
*  Bilastine
... a new selective histamine H1 receptor antagonist: Receptor selectivity and in vitro antihistaminic activity". Drugs in R&D. 6 ( ... Bilastine binds to guinea-pig cerebellar histamine H1-receptors (Ki=44 nM) and to human recombinant histamine H1-receptors (Ki= ... a new selective histamine H1 receptor antagonist. Receptor selectivity and in vitro antihistaminic activity". Drugs RD. 6 (6): ... It exerts its effect as a selective histamine H1 receptor antagonist, and has an effectiveness similar to cetirizine, ...
*  Cyclizine
... is a piperazine derivative with histamine H1-receptor antagonist (antihistamine) activity. The precise mechanism of ...
*  Hydroxyzine
"Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models". European Journal of ... "Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4- ... Hydroxyzine's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action ... Simons FE, Simons KJ, Frith EM (January 1984). "The pharmacokinetics and antihistaminic of the H1 receptor antagonist ...
*  Tripelennamine
Oishi R, Shishido S, Yamori M, Saeki K (February 1994). "Comparison of the effects of eleven histamine H1-receptor antagonists ... "Potentiation of L-dopa-induced behavioral excitement by histamine H1-receptor antagonists in mice". Japanese Journal of ... Tripelennamine acts primarily as an antihistamine, or H1 receptor antagonist. It has little to no anticholinergic activity.[ ...
*  Date rape drug
... chloral hydrate and some histamine H1 antagonists, common recreational drugs such as ethanol, marijuana, cocaine, and less ...
*  Alcaftadine
It is a H1 histamine receptor antagonist. It was approved by the U.S. Food and Drug Administration in 2010 under the trade name ... Alcaftadine is an antagonist at three of the histamine receptors (1, 2 and 4). The main indication for Alcaftadine is for ... This effect on histamine receptors seems to show lower rates of itching, eosinophil recruitment and redness after exposure to ...
*  Muscarinic acetylcholine receptor M2
... histamine H1 antagonist Otenzepad - 11-([2-[(Diethylamino)methyl]-1-piperidinyl]acetyl)-5,11-dihydro-6H-pyrido[2,3-b][1,4] ... mixed M2/M4 antagonist) - N-[2-[2-[(Dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4] ... and a number of selective M2 antagonists are available. methacholine (selective m3 muscarinic agonist) Iper-8-naph (compound 8b ... a new cardioselective M-2 muscarinic receptor antagonist, alone and in combination with atropine and gallamine". Eur. J. ...
*  Pseudoephedrine/loratadine
Loratadine is a long-acting antihistamine (H1 histamine antagonist) that is less sedating than older substances of its type. ...
*  CYP3A4
Often this allows prodrugs to be activated and absorbed - as in the case of the histamine H1-receptor antagonist terfenadine. ...
*  Pressing
... , a generic drug name of Hemofarm Group for Loratadine, a second-generation H1 histamine antagonist drug used to treat ...
*  Brompheniramine
... works by acting as an antagonist of histamine H1 receptors. It also functions as a moderately effective ...
*  Histamine
... neurons increase wakefulness and prevent sleep. Classically, antihistamines (H1 histamine receptor antagonists) which ... Histamine intolerance Histamine receptor antagonist Red wine headache Scombroid food poisoning Histamine Material Safety Data ... In humans, histamine exerts its effects primarily by binding to G protein-coupled histamine receptors, designated H1 through H4 ... In aqueous solution, histamine exists in two tautomeric forms: Nπ-H-histamine and Nτ-H-histamine. The imidazole ring has two ...
*  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. ...
*  Carbinoxamine
... is a histamine antagonist, specifically an H1-antagonist. The maleic acid salt of the levorotatory isomer is sold ...
*  Antiemetic
H1 histamine receptor antagonists) are effective in many conditions, including motion sickness, morning sickness in pregnancy, ... is an antidepressant that also has antiemetic effects and is also a potent histamine H1 receptor antagonist, Ki=1.6 nM. ... also a 5-HT3 receptor antagonists NK1 receptor antagonist Aprepitant (Emend) is a commercially available NK1 Receptor ... Dopamine antagonists act in the brain and are used to treat nausea and vomiting associated with neoplastic disease, radiation ...
*  Imipramine
Histamine: imipramine is an antagonist of the histamine H1 receptors. BDNF: BDNF is implicated in neurogenesis in the ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (2012). "Interactions of recombinant human histamine H₁R, H₂R, H₃R, ... histamine, and cholinergic receptors. Imipramine was discovered in 1951 and was introduced for medical use in 1957. It was the ... specifically an antagonist of the muscarinic acetylcholine receptors. Thus, it is prescribed with caution to the elderly and ...
*  Dexchlorpheniramine
... is an antihistamine, or an antagonist of the histamine H1 receptor. A study found that dexchlorpheniramine ...
*  Bepotastine
It is a direct H1-receptor antagonist that inhibits the release of histamine from mast cells. The ophthalmic formulation has ... and olopatadine on histamine-induced wheal-and flare-response, sedation, and psychomotor performance". Clinical and ...
*  Antihistamine
H1-antihistamines can be either neutral receptor antagonists or inverse agonists. Normally, histamine binds to the H1 receptor ... Research into these drugs led to the discovery that they were H1 antagonists and also to the development of H2 antagonists, ... H1-antihistamines refer to compounds that inhibit the activity of the H1 receptor. Since the H1 receptor exhibits constitutive ... like H1-antihistamines, occur as inverse agonists and neutral antagonists. They act on H2 histamine receptors found mainly in ...