The design, synthesis and pharmacological characterization of novel β₂-adrenoceptor antagonists.

ABSTRACT:

Background and purpose

Selective and potent antagonists for the β(2) -adrenoceptor are potentially interesting as experimental and clinical tools, and we sought to identify novel ligands with this pharmacology.

Experimental approach

A range of pharmacological assays was used to assess potency, affinity, selectivity (β(2) -adrenoceptor vs. β(1) -adrenoceptor) and efficacy.

Key results

Ten novel compounds were identified but none had as high affinity as the prototypical β(2) -adrenoceptor blocker ICI-118,551, although one of the novel compounds was more selective for β(2) -adrenoceptors. Most of the ligands were inverse agonists for β(2) -adrenoceptor-cAMP signalling, although one (5217377) was a partial agonist and another a neutral antagonist (7929193). None of the li

SUBMITTER: Hothersall JD 

PROVIDER: S-EPMC3174413 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature