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*  Histamine H2 receptor
The drug betazole is an example of a histamine H2 receptor agonist. Histamine is a ubiquitous messenger molecule released from ... Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin- ... Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253-78. PMID 9311023. "Entrez Gene: HRH2 histamine ... Experimental histamine H2 receptor agonist used for asthma and COPD) Inhibit antibody synthesis, T-cell proliferation and ...
*  Histamine H1 receptor
... is promoted by the constitutive activity of the H1 receptor as well as by agonists that bind at the receptor. H1-antihistamines ... 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 ... Horváth BV, Szalai C, Mándi Y, László V, Radvány Z, Darvas Z, Falus A (Nov 1999). "Histamine and histamine-receptor antagonists ...
*  Histamine agonist
... paradoxically histamine increasing). Histamine antagonist Histamine agonist at the US National Library of Medicine Medical ... 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. H3 : Betahistine is a weak ... Histamine1 agonist and a very strong Histamine3 antagonist ( ...
*  Immethridine
... 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. ...
*  VUF-8430
... is a histamine agonist selective for the H4 subtype. Smith FM, Haskelberg H, Tracey DJ, Moalem-Taylor G (2007). "Role ... 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): ...
*  Amthamine
... 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 ...
*  Alpha-Methylhistamine
α-Methylhistamine is a histamine agonist selective for the receptor subtype H3. It causes lowering of blood pressure and a ... "Production by R-alpha-methylhistamine of a histamine H3 receptor-mediated decrease in basal vascular resistance in guinea-pigs ...
*  OUP-16
... is a histamine agonist selective for the H4 subtype. Hashimoto, T; Harusawa, S; Araki, L; Zuiderveld, OP; Smit, MJ; ... "A Selective Human H4-Receptor Agonist: (−)-2-Cyano-1-methyl-3-{(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-yl} ...
*  4-Methylhistamine
... 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): ...
*  2-Pyridylethylamine
... is a histamine agonist which is selective for the H1 subtype. CID 75919 from PubChem Flynn SB, Gristwood RW ... and H2-receptors in the mediation of the effects of histamine in the isolated working heart of the guinea-pig". Br. J. ... Owen DA (January 1979). "Differentiation of the roles of histamine H1- ...
*  Methimepip
... 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- ...
*  Impromidine
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. ...
*  Histamine trifluoromethyl toluidide
... (HTFMT) is a mixed H1/H2 histamine agonist which is significantly more potent than ... Effects of histamine-trifluoromethyl-toluidide derivative (HTMT) on intracellular calcium in human lymphocytes. Journal of ... It also produces additional actions which appear to be independent of histamine receptors. Whyment AD, Blanks AM, Lee K, Renaud ... Inhibition of store-operated calcium entry-mediated superoxide generation by histamine trifluoromethyltoluide independent of ...
*  Histaminergic
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. ...
*  Imetit
... 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 ...
*  Dimaprit
... 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 ...
*  Immepip
... is a histamine H3 receptor agonist. Cannon KE, Leurs R, Hough LB (2007). "Activation of peripheral and spinal histamine ...
*  Betazole
... (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. ...
*  H3 receptor antagonist
In the beginning of development for H3R ligands the focus was on the agonist histamine which contains an imidazole ring in its ... Histamine plays a well documented role in AD, however 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: ... "Discovery of novel steroidal histamine H 3 receptor antagonists/inverse agonists". Bioorganic & Medicinal Chemistry Letters. 27 ...
*  Ciproxifan
... 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 ...
*  Chlorphenamine
It is specifically a potent inverse agonist of the histamine H1 receptor. The drug is also commonly described as possessing ... In addition to being a histamine H1 receptor antagonist, chlorphenamine has been found to act as a potent serotonin reuptake ... Suessbrich H, Waldegger S, Lang F, Busch AE (1996). "Blockade of HERG channels expressed in Xenopus oocytes by the histamine ... Arias-Montaño JA, Young JM (1993). "Characteristics of histamine H1 receptors on HeLa cells". Eur. J. Pharmacol. 245 (3): 291-5 ...
*  List of MeSH codes (D16)
... histamine agonists MeSH D27.505.519.625.375.425 --- histamine antagonists MeSH D27.505.519.625.375.425.400 --- histamine h1 ... histamine agonists MeSH D27.505.696.577.375.425 --- histamine antagonists MeSH D27.505.696.577.375.425.400 --- histamine h1 ... adrenergic alpha-agonists MeSH D27.505.519.625.050.100.200 --- adrenergic beta-agonists MeSH D27.505.519.625.050.200 --- ... adrenergic alpha-agonists MeSH D27.505.696.577.050.100.200 --- adrenergic beta-agonists MeSH D27.505.696.577.050.200 --- ...
*  Diphenhydramine
... acts primarily as an inverse agonist of the histamine H1 receptor. It is a member of the ethanolamine class of ... Histamine, Bradykinin, and Their Antagonists". In Brunton L. Goodman & Gilman's The Pharmacological Basis of Therapeutics (12e ... Krystal AD, Richelson E, Roth T (2013). "Review of the histamine system and the clinical effects of H1 antagonists: basis for a ... By reversing the effects of histamine on the capillaries, it can reduce the intensity of allergic symptoms. It also crosses the ...
*  GSK-189,254
... is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar ... Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat ... The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. British Journal of Pharmacology. 2008 ... Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and ...
*  Desloratadine
... is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor. At very high ...
*  Nonsteroidal antiandrogen
Cimetidine (Tagamet): An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR ... "Non-steroidal antiandrogen monotherapy compared with luteinizing hormone-releasing hormone agonists or surgical castration ...
*  Loratadine
... which acts as a selective inverse agonist of peripheral histamine H1-receptors. The potency of second generation histamine ...