Chemistry:ICI-118,551
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| IUPAC name
3-(isopropylamino)-1-[(7-methyl-4-indanyl)oxy]butan-2-ol
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| Identifiers | |
3D model (JSmol)
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| ChEMBL | |
| MeSH | ICI+118551 |
PubChem CID
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| Properties | |
| C17H27NO2 | |
| Molar mass | 277.402 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
 verify (what is   ?)
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| Infobox references | |
ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker.[1][2] ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, 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.
ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β2 adrenergic receptor, as few other specific antagonists for this receptor are known.[5] ICI-118,551 has been used in pre-clinical studies using murine models.[6][7][8] When dissolved in saline, the compound crosses the blood–brain barrier. Common systemic doses used in rodent research are 0.5 or 1 mg/kg although efficacy has been demonstrated at doses as low as 0.0001 mg/kg (100 ng/kg) in rhesus monkeys.[9] 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
- ↑ "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. August 2005. doi:10.1124/jpet.105.084947. PMID 15908513.
- ↑ "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. 2008. doi:10.1016/j.vascn.2008.06.003. PMID 18652905.
- ↑ "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. May 1988. doi:10.1016/S0022-2275(20)38502-3. PMID 2900871. http://www.jlr.org/cgi/pmidlookup?view=long&pmid=2900871.
- ↑ "Molecular characterization of the human beta 3-adrenergic receptor". Science 245 (4922): 1118–21. September 1989. doi:10.1126/science.2570461. PMID 2570461. Bibcode: 1989Sci...245.1118E.
- ↑ Adrenoceptors: Structure, Function. and Pharmacology.. Luxembourg: Harwood Academic Publisher. 1995.
- ↑ "Beta blocker use correlates with better overall survival in metastatic melanoma patients and improves the efficacy of immunotherapies in mice". Oncoimmunology 7 (3): e1405205. 21 December 2017. doi:10.1080/2162402X.2017.1405205. PMID 29399407.
- ↑ "Administration of a selective β2 adrenergic receptor antagonist exacerbates neuropathology and cognitive deficits in a mouse model of Alzheimer's disease". Neurobiology of Aging 35 (12): 2726–2735. December 2014. doi:10.1016/j.neurobiolaging.2014.06.011. PMID 25034342.
- ↑ "Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic beta2-adrenoceptor activation". British Journal of Pharmacology 127 (5): 1099–104. July 1999. doi:10.1038/sj.bjp.0702645. PMID 10455254.
- ↑ "Adrenergic pharmacology and cognition: focus on the prefrontal cortex". Pharmacology & Therapeutics 113 (3): 523–36. March 2007. doi:10.1016/j.pharmthera.2006.11.006. PMID 17303246.
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