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

... is a histamine agonist selective for the H2 subtype. It has been used in vitro and in vivo to study gastric secretion ... Eriks, J. C; Van Der Goot, H; Sterk, G. J; Timmerman, H (1992). "Histamine H2-receptor agonists. Synthesis, in vitro ... Coruzzi G, Timmerman H, Adami M, Bertaccini G (July 1993). "The new potent and selective histamine H2 receptor agonist ... Ezeamuzie, C. I; Philips, E (2000). "Histamine H(2) receptors mediate the inhibitory effect of histamine on human eosinophil ...

... is a histamine H3 receptor agonist. Garbarg, M; Arrang, JM; Rouleau, A; Ligneau, X; Tuong, MD; Schwartz, JC; Ganellin, ... CR (1992). "S-2-(4-imidazolyl)ethylisothiourea, a highly specific and potent histamine H3 receptor agonist". The Journal of ...

... is a histamine H3 receptor agonist. Cannon KE, Leurs R, Hough LB (2007). "Activation of peripheral and spinal histamine ...

Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). Subdivisions of histamine ... 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. ...

In the beginning of development for H3R ligands the focus was on the agonist histamine which contains an imidazole ring in its ... Though histamine plays a well documented role in AD, the varying levels of histamine in different areas of the brain make it ... Vohora, Divya; Bhowmik, Malay (2012). "Histamine H3 receptor antagonists/inverse agonists on cognitive and motor processes: ... H3R ligands have now been classified as agonists, antagonists or inverse agonists, depending on the signaling assay used. The ...

The drug betazole is an example of a histamine H2 receptor agonist. Histamine is a ubiquitous messenger molecule released from ... Inhibition of neutrophil activation and chemotaxis H2-receptor antagonist Histamine H1-receptor Histamine H3-receptor Histamine ... Histamine may play a role in penile erection. Histamine H2 receptors are expressed in the following tissues: Peripheral tissues ... Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin- ...

... which enhances histamine release in hypothalamus. An inverse agonist of the histamine H3 is Pitolisant. Results after testing ... A promising therapy would be to increase the activation of histaminergic neurons by an inverse agonist of the histamine H3 ... Its main target is the dopaminergic system because at pharmacological concentrations it acts as an agonist and modulates the ... Schwartz, Jean-Charles (2011). "The histamine H3 receptor: from discovery to clinical trials with pitolisant: H3 Receptor: from ...

... is a histamine agonist selective for the H3 subtype. Kitbunnadaj, R; Zuiderveld, OP; Christophe, B; Hulscher, S; ... and highly selective histamine H(3) receptor agonist". Journal of Medicinal Chemistry. 47 (10): 2414-7. doi:10.1021/jm049932u. ... Histamine agonists, Imidazoles, 4-Pyridyl compounds, All stub articles, Pharmacology stubs). ...

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 ... 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 ...

... is an extremely potent histamine H3 inverse agonist/antagonist. The histamine H3 receptor is an inhibitory ... a histamine H3-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat ... Histamine has an excitatory effect in the brain via H1 receptors in the cerebral cortex, and so drugs such as ciproxifan which ... Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (December 2004). "The histamine H3 receptor as a novel therapeutic target ...

... is a histamine agonist selective for the H4 subtype. Hashimoto, T; Harusawa, S; Araki, L; Zuiderveld, OP; Smit, MJ; ... Histamine agonists, Nitriles, Tetrahydrofurans, Imidazoles, All stub articles, Pharmacology stubs). ... "A Selective Human H4-Receptor Agonist: (−)-2-Cyano-1-methyl-3-{(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-yl} ...

D2-receptor agonists, D3 receptor agonists, D4 receptor agonists, Dopamine receptor modulators, Ergolines, Histamine agonists, ... Lisuride is a partial agonist of the D2, D3, D4, 5-HT2A, 5-HT2C, 5-HT5A, and H1 receptors, a full or near-full agonist of the 5 ... March 2004). "8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist". Molecular Pharmacology. 65 (3): ... Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal ...

... is a histamine agonist selective for the H4 subtype. Smith FM, Haskelberg H, Tracey DJ, Moalem-Taylor G (2007). "Role ... Histamine agonists, Guanidines, Thioureas, All stub articles, Amine stubs, Pharmacology stubs). ... as a potent nonimidazole histamine H4 receptor agonist". Journal of Medicinal Chemistry. 49 (23): 6650-1. doi:10.1021/jm060880d ... of histamine H3 and H4 receptors in mechanical hyperalgesia following peripheral nerve injury". Neuroimmunomodulation. 14 (6): ...

... (also known as ametazole) is a histamine H2 receptor agonist. Betazole hydrochloride is known as gastramine and ... It therefore does not require concomitant use of antihistaminic compounds to block the actions of histamine at other histamine ... Betazole is used as a stimulant in preference to histamine because of its specificity for the H2 receptor and its advantage of ... not generating the undesirable side effects that histamine would induce. ...

... is a histamine agonist selective for the H4 subtype. Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, ... Leurs R (September 2005). "Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: ... identification of 4-methylhistamine as the first potent and selective H4 receptor agonist". J. Pharmacol. Exp. Ther. 314 (3): ...

It is specifically a potent inverse agonist of the histamine H1 receptor. The drug is also commonly described as possessing ... In addition to acting as an inverse agonist at the H1 receptor, chlorphenamine has been found to act as a serotonin reuptake ... Arias-Montaño JA, Young JM (May 1993). "Characteristics of histamine H1 receptors on HeLa cells". European Journal of ... Yasuda SU, Wellstein A, Likhari P, Barbey JT, Woosley RL (August 1995). "Chlorpheniramine plasma concentration and histamine H1 ...

... is a histamine agonist selective for the receptor subtype H3. It causes lowering of blood pressure and a ... Histamine agonists, All stub articles, Cardiovascular system drug stubs). ... "Production by R-alpha-methylhistamine of a histamine H3 receptor-mediated decrease in basal vascular resistance in guinea-pigs ...

Histamine agonists Durant G, Duncan W, Ganellin C, Parsons M, Blakemore R, Rasmussen A (1978). "Impromidine (SK&F 92676) is a ... Impromidine (INN) is a highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric ... very potent and specific agonist for histamine H2 receptors". Nature. 276 (5686): 403-5. doi:10.1038/276403a0. PMID 714166. ...

Other treatments which have been used include atypical antipsychotics, histamine receptor antagonists, and dopamine agonists. ...

... is a histamine agonist which is selective for the H1 subtype. Flynn SB, Gristwood RW, Owen DA (January 1979 ... Histamine agonists, 2-Pyridyl compounds, All stub articles, Amine stubs, Heterocyclic compound stubs). ... "Differentiation of the roles of histamine H1- and H2-receptors in the mediation of the effects of histamine in the isolated ...

... is a histamine analog working as a selective H2 histamine receptor agonist. Kartzung, Betram G.; Trevor, Anthony J., ... a Histamine H2-agonist, Inhibits Anaphylactic Histamine Release from Mast Cells and the Decreased Release is Restored by ... "Efficacy of a Selective Histamine H2 Receptor Agonist, Dimaprit, in Experimental Models of Endotoxin Shock and Hepatitis in ...

It acts as an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other ... It is classified as a second-generation antihistamine and works by blocking histamine H1-receptors. Levocetirizine was approved ... and dextrocetirizine on histamine-induced nasal response in healthy adult volunteers". Allergy. 56 (4): 339-343. doi:10.1034/j. ... and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers". Allergy. 56 (1): 50-57. doi:10.1034/j.1398 ...

... is a histamine agonist which is highly selective for the H3 subtype. It is the N-methyl derivative of immepip. ... discovery of methimepip as a potent and selective histamine H3 receptor agonist". Journal of Medicinal Chemistry. 48 (6): 2100- ... Histamine agonists, Piperidines, All stub articles, Pharmacology stubs). ...

... acts primarily as an antagonist or inverse agonist of the histamine H1 receptor. This action is responsible for its ... Doxylamine is an antihistamine-specifically an inverse agonist of the histamine H1 receptor-and to a lesser extent an ... Krystal AD, Richelson E, Roth T (August 2013). "Review of the histamine system and the clinical effects of H1 antagonists: ... Simons FE, Simons KJ (December 2011). "Histamine and H1-antihistamines: celebrating a century of progress". The Journal of ...

GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar ... August 2008). "Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and ... Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: an attractive ... June 2007). "GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and ...

... 's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action ... Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (September 2005). "Evaluation of histamine H1-, H2-, and H3- ... Hydroxyzine works by blocking the effects of histamine. It is a first-generation antihistamine in the piperazine family of ... Yanai K, Tashiro M (January 2007). "The physiological and pathophysiological roles of neuronal histamine: an insight from human ...

... analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists". Biochemical Pharmacology. 71 (8): 1103-13. ... ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and has been ... inverse agonists. Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, Marsh K, ... Potent and selective histamine H3 receptor antagonist with drug-like properties". J. Pharmacol. Exp. Ther. 313 (1): 165-75. doi ...

... is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor. At very high ... Desloratadine (trade names Clarinex and Aerius) is a tricyclic H1 inverse agonist that is used to treat allergies. It is an ...

... which acts as a selective inverse agonist of peripheral histamine H1 receptors. The potency of second generation histamine ...