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
^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.
PMID15908513.
S2CID12446381.
^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.
PMID18652905.
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
^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.
PMID15908513.
S2CID12446381.
^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.
PMID18652905.