1 -Arylpiperazinyl -4 -cyclohexylamine derived isoindole-1,3-diones as potent and selective α-1a/1d adrenergic receptor ligands

Abstract Subtype-selective α-1a and/or α-1d adrenergic receptor antagonists may be useful for the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) with fewer adverse effects than non-selective drugs. A series of 1-arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones has been synthesized, displaying in vitro α 1a and α 1d binding affinity K i values in the range of 0.09–38 nM with K i (α 1b )/ K i (α 1a ) and K i (α 1b )/ K i (α 1d ) selectivity ratios up to 3607-fold.