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

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.beta blocker Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms ( arrhythmia), and to protect the heart from a second heart attack after a first heart attack ( secondary prevention ...

. ICI binds to the β₂ subtype with at least 100 times greater

affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ...

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 industry, chemical company. It was, for much of its history, the largest manufacturer in Britain. Its headquarters were at Millbank in London. ICI was listed on the London Stock Exchange ...

, which was acquired by

AkzoNobel Akzo Nobel N.V., stylised as AkzoNobel, is a Dutch multinational corporation, multinational company which creates paints and performance coatings for both industry and consumers worldwide. Headquartered in Amsterdam, the company has activities ...

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: Salt-related * Saline (medicine), a liquid with salt content to match the human body * Saline water, non-medicinal salt water * Saline, a historical term (especially American) for a salt works or saltern Places United States ...

, 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 regulates the transfer of solutes and chemicals between the circulatory system and the central nervous system ...

. 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 The rhesus macaque (''Macaca mulatta''), colloquially rhesus monkey, is a species of Old World monkey. There are between six and nine recognised subspecies split between two groups, the Chinese-derived and the Indian-derived. Generally brown or ...

. 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 Secondary amines Isopropylamino compounds