PipISB

From Wikipedia, the free encyclopedia
Jump to: navigation, search
PipISB
PipISB structure.png
Systematic (IUPAC) name
N-(4-fluorobenzyl)-4-(3-(piperidin-1-ylindole-1-sulfonyl)benzamide
Clinical data
Legal status ?
Identifiers
ATC code ?
PubChem CID 58975213
Chemical data
Formula C27H26FN3O3S 
Mol. mass 491.58

PipISB is a drug used in scientific research which acts as a potent and selective inverse agonist of the cannabinoid receptor CB1. It is highly selective for the CB1 receptor over CB2, with a Kd at CB1 of 1.5nM vs over 7000nM at CB2, has good blood-brain barrier penetration, and can be conveniently radiolabelled with either 11C or 18F, making it useful for mapping the distribution of CB1 receptors in the brain.[1][2]


References[edit]

  1. ^ Donohue, Sean R.; Halldin, Christer; Schou, Magnus; Hong, Jinsoo; Phebus, Lee; Chernet, Eyassu; Hitchcock, Stephen A.; Gardinier, Kevin M.; Ruley, Kevin M.; Krushinski, Joseph H.; Schaus, John; Pike, Victor W. (2008). "Radiolabeling of a high potency cannabinoid subtype-1 receptor inverse agonist, N-(4-fluoro-benzyl)-4-(3-(piperidin-1-yl-indole-1-sulfonyl)benzamide (PipISB), with carbon-11 or fluorine-18". Journal of Labelled Compounds and Radiopharmaceuticals 51 (3): 146. doi:10.1002/jlcr.1491.  edit
  2. ^ Finnema, S. J.; Donohue, S. R.; Zoghbi, S. S.; Brown, A. K.; Gulyás, B. Z.; Innis, R. B.; Halldin, C.; Pike, V. W. (2009). "Evaluation of \11C]PipISB and \18F]PipISB in monkey as candidate radioligands for imaging brain cannabinoid type-1 receptors in vivo". Synapse 63 (1): 22–30. doi:10.1002/syn.20578. PMC 2587077. PMID 18925657.  edit