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Cipralisant
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| Systematic (IUPAC) name | |
| (1S,2S)-4-(2-(5,5-dimethylhex-1-ynyl) cyclopropyl)imidazole |
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| 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;314(1):271-81. PMID 15821027
- ^ An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute Configuration
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- This page was last modified on 1 August 2008, at 02:51.
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