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| Formula | C14H20N2 |
| Molar mass | 216.328 g·mol−1 |
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Cipralisant (GT-2331, tentative trade namePerceptin) is an extremely potenthistamine H3 receptor ligand originally developed by Gliatech.[1] Cipralisant was initially classified as a selective H3antagonist,[2] but newer research (2005) suggests alsoagonist properties, i.e.,functional selectivity.[3]
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, showingfunctional selectivity and stimulating one type ofG-protein coupled pathway while failing to activate other intracellular pathways.[3]
Gliatech filed for bankruptcy in 2002, and its intellectual property was inherited byMerck. 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.[4]
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