Cipralisant

Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent histamine H3 receptor ligand originally developed by Gliatech. Cipralisant was initially classified as a selective H3 antagonist, but newer research (2005) suggests also agonist properties, i.e., functional selectivity.

"Perceptin" redirects here. For the robotics company PerceptIn, see Robotic vacuum cleaner.
Cipralisant
Clinical data
ATC code
  • none
Identifiers
  • 5-[(1S,2S)-2-(5,5-dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC14H20N2
Molar mass216.328 g·mol−1
3D model (JSmol)
  • CC(C)(C)CCC#C[C@H]1C[C@@H]1c2cnc[nH]2
  • InChI=1S/C14H20N2/c1-14(2,3)7-5-4-6-11-8-12(11)13-9-15-10-16-13/h9-12H,5,7-8H2,1-3H3,(H,15,16)/t11-,12-/m0/s1 N
  • Key:CVKJAXCQPFOAIN-RYUDHWBXSA-N N
 NY (what is this?)  (verify)

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.

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.

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