ICI-118,551 is a selective β₂ adrenergic receptor (adrenoreceptor)

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

or beta blocker. 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. The compound was developed by

Imperial Chemical Industries Imperial Chemical Industries (ICI) was a British chemical company. It was, for much of its history, the largest manufacturer in Britain. It was formed by the merger of four leading British chemical companies in 1926. Its headquarters were at M ...

, 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. ICI-118,551 has been used in pre-clinical studies using murine models. When dissolved in

saline Saline may refer to: * Saline (medicine), a liquid with salt content to match the human body * Saline water, non-medicinal salt water * Saline, a historical term (especially US) for a salt works or saltern Places * Saline, Calvados, a commune in ...

, the compound crosses the

blood–brain barrier The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that prevents solutes in the circulating blood from ''non-selectively'' crossing into the extracellular fluid of ...

. 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. 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

{{Adrenergics Secondary alcohols Beta blockers Indanes Phenol ethers Amines Isopropylamino compounds