Cipralisant

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.

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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