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Cipralisant



Cipralisant
Systematic (IUPAC) name
(1R,2R)-4-(2-(5,5-dimethylhex-1-ynyl)
cyclopropyl)imidazole
Identifiers
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Chemical data
Formula C14H20N2 
Mol. mass 216.32 g/mol
Pharmacokinetic data
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Therapeutic considerations
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Legal status
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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.

Additional recommended knowledge

Gliatech filed for bankruptcy in 2002, and its intellectual property inherited by Merck. The development of cipralisant seems to have been suspended since 2003.


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
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Cipralisant". A list of authors is available in Wikipedia.
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