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20-September-2008 09:55:57 - Cipralisant Cipralisant Systematic IUPAC name 1S,2S-4-2-5,5-dimethylhex-1-ynyl cyclopropylimidazole Identifiers CAS number ? ATC code ? PubChem ? Chemical data Formula C14H20N2 Mol. mass 216.32 g/mol Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? Cipralisant GT-2331, tentative trade name Perceptin is an extremely potent Histamine H3 receptor ligand originally developed by Gliatech.1 Cipralisant was initially classified as a selective H3 antagonist, and seemed to be well tolerated during early testing, entering Phase II trials for ADHD in 2000. The relatively recent cloning of human H3 receptor, as well as the discovery of its constitutive activity provided the ability to better assess the activity of H3 receptor ligands. Consequently cipralisant was reassessed as an H3 receptor agonist in human and rat recombinant systems, showing functional selectivity and stimulating one type of G-protein coupled pathway while failing to activate other intracellular pathways.2 Gliatech filed for bankruptcy in 2002, and its intellectual property was inherited by Merck. The development of cipralisant seems to have been suspended since 2003 but research is ongoing, and recently it has been shown that it is the 1S,2S enantiomer which is the biologically active one.3 References ^ Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor ^ Krueger KM, Witte DG, Ireland-Denny L, Miller TR, Baranowski JL, Buckner S, Milicic I, Esbenshade TA, Hancock AA. G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations. Journal of Pharmacology and Experimental Therapeutics. 2005 Jul;3141:271-81. PMID 15821027 ^ An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute Configuration Tablets This pharmacology-related article is a stub. v d e Histamine agonists H1 2-Pyridylethylamine H2 Amthamine - Betazole - Dimaprit - Impromidine H3 α-methylhistamine - Cipralisant - Imetit - Immepip - Immethridine - Methimepip - Proxyfan H4 4-Methylhistamine - VUF-8430 Unselective Betahistine - Histamine - Histamine trifluoromethyl toluidide Retrieved from http://en..org/wiki/Cipralisant Categories: Pharmacology stubs | Histamine agonists Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 1 August 2008, at 02:51
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