View source for ICI-118,551

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|ImageFile=ICI 118551.svg
|ImageSize=
|IUPACName=3-(isopropylamino)-1-[(7-methyl-4-indanyl)oxy]butan-2-ol
|OtherNames=
|Section1={{Chembox Identifiers
|  CASNo=72795-19-8
|  PubChem=3682
|  SMILES=CC1=C2CCCC2=C(C=C1)OCC(C(C)NC(C)C)O
|  MeSHName=ICI+118551
  }}
|Section2={{Chembox Properties
|  Formula=C<sub>17</sub>H<sub>27</sub>NO<sub>2</sub>
|  MolarMass=277.402 g/mol
|  Appearance=
|  Density=
|  MeltingPt=
|  BoilingPt=
|  Solubility=
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|Section3={{Chembox Hazards
|  MainHazards=
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  }}
}}

'''ICI-118,551''' is a selective [[beta-2 adrenergic receptor|beta-2]] (β<sub>2</sub>) [[adrenergic receptor]] [[receptor antagonist|antagonist]].<ref name="pmid15908513">{{cite journal |author=Hillman KL, Doze VA, Porter JE |title=Functional characterization of the beta-adrenergic receptor subtypes expressed by CA1 pyramidal cells in the rat hippocampus |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=314 |issue=2 |pages=561–7 |year=2005 |month=August |pmid=15908513 |doi=10.1124/jpet.105.084947}}</ref><ref name="pmid18652905">{{cite journal |author=Summerhill S, Stroud T, Nagendra R, Perros-Huguet C, Trevethick M |title=A cell-based assay to assess the persistence of action of agonists acting at recombinant human beta(2) adrenoceptors |journal=Journal of Pharmacological and Toxicological Methods |volume=58 |issue=3 |pages=189–97 |year=2008 |pmid=18652905 |doi=10.1016/j.vascn.2008.06.003}}</ref> ICI binds to the β<sub>2</sub> subtype with at least 100 times greater [[Ligand (biochemistry)#Receptor/Ligand binding affinity|affinity]] than [[beta-1 adrenergic receptor|β<sub>1</sub>]] or [[beta-3 adrenergic receptor|β<sub>3</sub>]], the two other known subtypes of the beta adrenoceptor.<ref name="pmid2900871">{{cite journal |author=Mauriège P, De Pergola G, Berlan M, Lafontan M |title=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=Journal of Lipid Research |volume=29 |issue=5 |pages=587–601 |year=1988 |month=May |pmid=2900871 |url=http://www.jlr.org/cgi/pmidlookup?view=long&pmid=2900871}}</ref><ref name="pmid2570461">{{cite journal |author=Emorine LJ, Marullo S, Briend-Sutren MM, ''et al.'' |title=Molecular characterization of the human beta 3-adrenergic receptor |journal=Science |volume=245 |issue=4922 |pages=1118–21 |year=1989 |month=September |pmid=2570461 |doi=10.1126/science.2570461}}</ref> The compound was developed by [[Imperial Chemical Industries]], which was acquired by [[AkzoNobel]] in 2008. 

ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β<sub>2</sub> adrenergic receptor, as few other specific antagonists for this receptor are known.<ref> Ruffolo, Robert R. Jr. ed. 1995. Adrenoceptors: Structure, Function. and Pharmacology. Harwood Academic Publisher, Luxembourg.</ref> 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 macaque|rhesus monkeys]].<ref>{{cite journal |author=Ramos BP, Arnsten AF |title=Adrenergic pharmacology and cognition: focus on the prefrontal cortex |journal=Pharmacology & Therapeutics |volume=113 |issue=3 |pages=523–36 |year=2007 |month=March |pmid=17303246 |pmc=2151919 |doi=10.1016/j.pharmthera.2006.11.006}}</ref> 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==
{{reflist}}


{{Adrenergic antagonist}}

[[Category:Beta blockers]]
[[Category:Indanes]]
[[Category:Phenol ethers]]
[[Category:Alcohols]]
[[Category:2Fix]]