D-Isoleucine is a selective activator of Asc-1 antiporter, which enhances long-term potentiation at the hippocampal CA1-CA3 via release of endogenous D-serine.

Amylin (AMY3) antagonist (IC50 = 0.3 μM). Protects neuronal cells from Aβ(1-42)-induced cytotoxicity in vitro. Brain penetrant. Improves spatial memory and reduces Aβ plaque number and total area in a mouse Alzheimer's disease model.

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.