Cipralisant
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Cipralisant
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| Systematic (IUPAC) name | |
| (1R,2R)-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. |
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| Legal status | |
| Routes | ? |
Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent Histamine H3 receptor ligand originally developed by Gliatech. Cipralisant seemed to be well tolerated during early testing and it entered Phase II 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. Unfortunately, cipralisant was reassessed as an H3 receptor agonist in human and rat recombinant systems.
Gliatech filed for bankruptcy in 2002, and its intellectual property inherited by Merck. The development of cipralisant seems to have been suspended since 2003.
[edit] References
- Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor
- An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute Configuration
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