Description
ICI 118551 is a potent, selective antagonist of the β
2-
adrenergic receptor (Ki = 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
The (R,R)-enantiomer of ICI 118551 as highly selective β2-adrenoceptor antagonist. The S,S-enantiomer is the most potent.
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
Biochem/physiol Actions
ICI 118,551 has been used to treat vasomotor migraines and somatic troubles related to anxiety state.