The Full Wiki

More info on Cipralisant

Cipralisant: Wikis

Advertisements

Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.

Encyclopedia

From Wikipedia, the free encyclopedia

Cipralisant
Systematic (IUPAC) name
(1S,2S)-4-(2-(5,5-dimethylhex-1-ynyl)
cyclopropyl)imidazole
Identifiers
CAS number  ?
ATC code none
PubChem  ?
Chemical data
Formula C 14H20N2  
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

  1. ^ Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor
  2. ^ 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
  3. ^ An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute Configuration
Advertisements

Advertisements






Got something to say? Make a comment.
Your name
Your email address
Message