(±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanolhydrochloride Chemical Properties

storage temp. 

desiccated

solubility 

DMSO : 25 mg/mL (79.65 mM; Need ultrasonic)H2O : 12.5 mg/mL (39.83 mM; Need ultrasonic)

form 

powder

color 

white

Water Solubility 

H2O: >10mg/mL

Safety Information

WGK Germany 

3

(±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanolhydrochloride Usage And Synthesis

Description

ICI 118551 is a potent, selective antagonist of the β₂-adrenergic receptor (K_i = 0.7 nM for the β₂receptor, compared with 49.5 and 611 nM for β₁ and β₃ receptors, respectively). It is active in vivo and is often used to evaluate the actions of adrenergic receptor agonists.

Uses

ICI 118,551 hydrochloride has been used:

• to block β-adrenergic signaling in various experiments
• to counteract degradation by endogenous T-lymphocyte monoamine oxidases
• to determine the specific receptor subtype necessary for isoproterenol to induce up-regulation of gene transcripts

Uses

The (R,R)-enantiomer of ICI 118551 as highly selective β2-adrenoceptor antagonist. The S,S-enantiomer is the most potent.

Biochem/physiol Actions

ICI 118,551 has been used to treat vasomotor migraines and somatic troubles related to anxiety state.

in vivo

IC 50

β adrenergic receptor

storage

Store at RT

References

[1] N M DEIGHTON. Characterization of the beta adrenoceptor subtype(s) mediating the positive inotropic effects of epinine, dopamine, dobutamine, denopamine and xamoterol in isolated human right atrium.[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 262 2: 532-538.
[2] NANCY J. ROTHWELL  Deepak K S  Michael J Stock. Changes in tissue blood flow and β-receptor density of skeletal muscle in rats treated with the β2-adrenoceptor agonist clenbuterol[J]. British Journal of Pharmacology, 1987, 90 3: 601-607. DOI: 10.1111/j.1476-5381.1987.tb11211.x
[3] IL-MAN KIM. Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2008: 14555-14560. DOI: 10.1073/pnas.0804745105

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