Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate muscle in vitro and on intra-urethral pressure in rats.

Isosalvipuberulin is a natural product of Salvia, Lamiaceae. Isosalvipuberulin can be used as a reference standard.

Azelaprag (AMG 986) is an effective small-molecule apelin receptor agonist. Azelaprag can be used to treat neurological diseases and cardiovascular diseases.