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ICI-118,551
ICI 118551.svg
IUPAC name
Identifiers
CAS number 72795-19-8
PubChem 3682
MeSH ICI+118551
SMILES
Properties
Molecular formula C17H27NO2
Molar mass 277.402 g/mol
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

ICI-118,551 is a selective beta-2 antagonist.[1][2] ICI binds to the beta-2 subtype with at least 100 times greater affinity than beta-1 or beta-3, the two other known subtypes of the beta adrenoceptor.[3][4] The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008.

When dissolved in saline, the compound crosses the blood-brain barrier. Common systemic doses used in rodent research are .5 or 1 mg/kg although efficacy has been demonstrated at doses as low as .0001 mg/kg in rhesus monkeys.[5] Doses up to 20 mg/kg have been used without toxicity. At room temperature in saline, the ICI 118,551 hydrochloride is soluble to at least 2.5 mg/mL.

References

  1. ^ Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed by CA1 pyramidal cells in the rat hippocampus". The Journal of Pharmacology and Experimental Therapeutics 314 (2): 561–7. doi:10.1124/jpet.105.084947. PMID 15908513.  
  2. ^ Summerhill S, Stroud T, Nagendra R, Perros-Huguet C, Trevethick M (2008). "A cell-based assay to assess the persistence of action of agonists acting at recombinant human beta(2) adrenoceptors". Journal of Pharmacological and Toxicological Methods 58 (3): 189–97. doi:10.1016/j.vascn.2008.06.003. PMID 18652905.  
  3. ^ Mauriège P, De Pergola G, Berlan M, Lafontan M (May 1988). "Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic binding sites on human fat cell membranes with highly selective beta 1-antagonists". Journal of Lipid Research 29 (5): 587–601. PMID 2900871. http://www.jlr.org/cgi/pmidlookup?view=long&pmid=2900871.  
  4. ^ Emorine LJ, Marullo S, Briend-Sutren MM, et al. (September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science 245 (4922): 1118–21. doi:10.1126/science.2570461. PMID 2570461.  
  5. ^ Ramos BP, Arnsten AF (March 2007). "Adrenergic pharmacology and cognition: focus on the prefrontal cortex". Pharmacology & Therapeutics 113 (3): 523–36. doi:10.1016/j.pharmthera.2006.11.006. PMID 17303246.  
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