Therapeutics: Adrenergic receptor a1 (ADRA1)

In vitro and rat studies identified an iminopyridine-based ADRA1 antagonist that could help treat overactive bladder (OAB). Chemical synthesis and in vitro testing of iminopyridine analogs yielded a compound that bound ADRA1 with a Ki of 1.1 nM. In a rat model of chemically-induced OAB, the compound decreased bladder contractions compared with no treatment. In another rat model of OAB, the compound increased voiding intervals. Next steps could include testing the compound in various models of incontinence.

Kissei Pharmaceutical Co. Ltd., Allergan plc, Choongwae Pharma Corp., Daiichi Sankyo Co. Ltd. and Recordati S.p.A. market Rapaflo silodosin, an ADRA1 antagonist, to treat BPH and have the compound in registration to treat urolithiasis and Phase II testing to treat prostatitis. ...