Advanced search
Publication Cover
Expert Opinion on Therapeutic Patents Volume 10, 2000 - Issue 7
Submit an article Journal homepage
71
Views
25
CrossRef citations to date
0
Altmetric
Review

Histamine H3 receptor antagonists

Matthew J Tozer The James Black Foundation, 68 Half Moon Lane, London, SE24 9JE, UK. [email protected]
&
S Barret Kalindjian The James Black Foundation, 68 Half Moon Lane, London, SE24 9JE, UK. [email protected]
Pages 1045-1055 | Published online: 25 Feb 2005

Bibliography

  • ARRANG J-M, GARBARG M, SCHWARTZ J-C:-inhibition of brain histamine release mediated by a novel class (113) of histamine receptor. Nature (1983) 302:832–837.
  • ••The first description of the histamine H3 receptor.
  • ARRANG J-M, GARBARG M, LANCELOT J-C et al: Highly and selective ligands for histamine 113-receptors. Nature (1987) 327:117–123.
  • ••Thioperamide, the first highly potent H3 antagonist.
  • STARK H, SCHLICKER E, SCHUNACK W: Developments of 113-receptor antagonists. Drugs Fut. (1996) 21:507–520.
  • •A recommendable review on H3 antagonists.
  • LEURS R, BLANDINA P, TEDFORD C, TIMMERMAN H: potential of histamine 113 receptor and antagonists. TiPS (1998) 19:177–183.
  • •A useful review which summarises the contrasting possibili-ties for both H3 antagonists and agonists.
  • ARRANG J, GARBARG M, SCHWARTZ J-C: Autoinhibition of histamine synthesis mediated by presynaptic 113-receptors. Neuroscience (1987) 23:149–157.
  • The Histamine H3 Receptor - A Target for New Drugs. Leurs R, Timmerman H (Eds.), Elsevier, Amsterdam (1998).
  • ••An important collection of essays on histamine H3 research.
  • LEVI R, SMITH NCE: Histamine 113-receptors: a new frontier in myocardial ischemia. J. Pharmacol Exp. Ther. (2000) 292:825–830.
  • HALPERN MT: GT-2331 (Gliatech Inc). Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs (1999) 1:524–527.
  • •A useful summary of the development and properties of GT-2331 up to Phase I clinical trials.
  • LOVENBERG TW, ROLAND BL, WILSON SJ et al.: Cloning functional expression of the human histamine 113 receptor. Mol. Pharmacol. (1999) 55:1101–1107.
  • ••The first cloning of a histamine H3 receptor.
  • STARK H, PURAND K, LIGNEAU X et al.: Novelcarbamates as potent histamine 113 receptor antago-nists with high in vitro and oral in vivo activity. J. Med. Chem. (1996) 39:1157–1163.
  • WINDHORST AD, TIMMERMAN H, KLOK RP, MENGE WMPB, LEURS R, HERSCHEID JDM: Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine 113 receptor. Bioorg. Med. Chem. (1999) 7:1761–1767.
  • GOTO T, SAKASHITA H, MURAKAMI K, SUGIURA M, KONDO T, FUKAYA C: Novel histamine 113 receptor antagonists: synthesis and evaluation of formamide and S-methylisothiourea derivatives. Chem. Pharm. Bull. (1997) 45:305–311.
  • STARK H, HeLS A, LIGNEAU X et al: Development of FUB181, a selective histamine 113-receptor antagonist of high oral in vivo potency with 440-(arylalky-loxy)alky11-1H-imidazole structure. Arch. Pharm. (1998) 331:211–218.
  • KATHMANN M, SCHLICKER E, MARR I, WERTHWEIN S, STARK H, SCHUNACK W: Ciproxifan and chemically related compounds are highly potent and selective histamine 113-receptor antagonists. Naunyn-Schmiedeberg's Arch. Pharmacol (1998) 358:623–627.
  • STARK H, ELZ S, LIGNEAU X et al: Development of ciproxifan and related histamine 113 receptor antago-nists. 12th Camerino-Noordwijkerhout Symposium, Receptor Chemistry Towards the Third Millennium. Camerino, Italy (1999): Poster no. 31.
  • LIGNEAU X, LIN J-S, VANNI-MERCIER G et al.:Neurochemical and behavioral effects of ciproxifan, a potent histamine 113-receptor antagonist. J. Pharmacol Exp. Ther. (1998) 287:658–666.
  • VAN DER GOOT H, SCHEPERS MJP, STERK GJ, TIMMERMAN H: Isothiourea analogues of histamine as potent agonists or antagonists of the histamine 113-receptor. Eur. J. Med. Chem. (1992) 27:5 1 1–5 17.
  • LEURS R, KATHMANN M, VOLLINGA RC, MENGE WMPB,SCHLICKER E, TIMMERMAN H: Histamine homologues discriminating between two functional histamine 113 receptor assays. Evidence for 113 receptor Heteroge-neity? J. Pharmacol Exp.Ther. (1996) 276:1–7.
  • KRAUSE M, STARK H, SCHUNACK W: Medicinal chemistry of histamine 113 receptor agonists. In: The Histamine H3 Receptor - A Target for New Drugs. Leurs R, Timmerman H (Eds.), Elsevier, Amsterdam (1998):175–196.
  • ASLANIAN R, BROWN JE, SHIH N-Y et al.:44( 1H-Imidazol-4-yOmethylibenzamidines and benzylamidines: novel antagonists of the histamine 113 receptor. Bioorg. Med. Chem. Lett. (1998) 8:2263–2268.
  • TEDFORD CE, YATES SL, PAWLOWSKI GP et al. Pharma- characterization of GT-2016, a non-thiourea-containing histamine 113 receptor agonist: in vitro and vivo studies. J. Pharmacol. Exp. Ther. (1995) 275:598–604.
  • PHILLIPS JG, ALI SM: Medicinal chemistry of histamine 113 receptor antagonists. In: The Histamine H3 Receptor - A Target for New Drugs. Leurs R, Timmerman H (Eds.), Elsevier, Amsterdam (1998):197–222.
  • TEDFORD CE, HOFFMANN M, SEYEDI N et al: High potency of GT-2227 and GT-2331, new histamine 113 receptor antagonists, in two functional models. Eur. J. Pharmacol (1998) 351:307–311.
  • YATES SL, PHILLIPS JG, GREGORY R et al: Identification pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine 113 receptor ligands. J. Pharmacol Exp. Ther. (1999) 289:1151–1159.
  • ALI SM, TEDFORD CE, GREGORY R et al.: Design, and structure-activity relationships of acetylene-based histamine 113 receptor antagonists. J. Med. Chem. (1999) 42:903–909.
  • TEDFORD CE, PHILLIPS JG, GREGORY R et al.: Develop- of trans-2[1Himidazol-4-yl] cyclopropane derivatives as new high-affinity histamine 113 receptor ligands. J. Pharmacol Exp. Ther. (1999) 289:1160–1168.
  • TOZER MJ, HARPER EA, KALINDJIAN SB, PETHER MJ, SHANKLEY NP, WATT GF: From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine 113-receptor antagonists. Bioorg. Merl. Chem. Lett. (1999) 9:1825–1830.
  • TOZER MJ, BUCK IM, COOKE T, KALINDJIAN SB, MCDONALD IM, STEEL KIM: 4-Chlorobenzyl sulfona-mide and sulfamide derivatives of histamine homologues: the design of potent histamine 113 receptor antagonists. Bioorg. Merl. Chem. Lett. (1999) 9:3103–3108.
  • SCHLICKER E, KATHMANN M, BITSCHNAU H et al: Potencies of antagonists chemically related to iodoproxyfan at histamine 113 receptors in mouse brain cortex and guinea pig ileum: evidence for 113 receptor heterogeneity? Naunyn-Schmiedeberg's Arch. Pharmacol. (1996) 353:482–488.
  • WOLIN R, CONNOLLY M, AFONSO A et al: Novel 113 antagonists. Sulfonamide homologs of histamine. Bioorg. Merl. Chem. Lett. (1998) 8:2157–2162.
  • PLAZZI PV, BORDI F, MOR M et al.: Heteroarylamino- and heteroarylthioethyl imidazoles synthesis and 113 receptor affinity. Eur. J. Med. Chem. (1995) 30:881–889.
  • LINNEY ID, BUCK IM, HARPER EA et al.: The design, and structure-activity relationships of novel non-imidazole histamine 113 receptor antagonists. J. Med. Chem. (2000): in press.
  • CLITHEROW JW, BESWICK P, IRVING WJ et al.: Novel 1,2,4-oxadiazoles as potent and selective histamine 113 receptor antagonists. Bioorg. Merl. Chem. Lett. (1996) 6:833–838.
  • WEST RE, JR., ZWEIG A, SHIH N-Y, SIEGEL MI, EGAN RW, CLARK MA: Identification of two 113-histamine receptor subtypes. Mol. Pharmacol. (1990) 38:610–613.
  • TARDIVEL-LACOMBE J, ROULEAU A, HERON A et al.: Cloning and cerebral expression of the guinea pig histamine 113 receptor: evidence for two isoforms. NeuroReport (2000) 1 1:7 55–759.
  • •Molecular biological evidence for the existence of histamine H3 receptor subtypes.

Websites

  • Gliatech, Inc. Press Release. (29th September 1999). http : //www . gliatech .com/news/newsread .cfm?ID 176 (May 2000).
  • Gliatech, Inc. Press Release. (13th December 1995). http:www.iddb.com/ 193478, Current Drugs Ltd. (May 2000).
  • Gliatech, Inc. Press Release. (27th February 1997). IDdb 235764, Current Drugs Ltd. (May 2000).
  • Gliatech, Inc. Press Release. (22nd November 1999). http : //www . gliatech .com/news/newsread .cfm?ID 182 (May 2000).

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.