Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.

Abstract A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT 2A receptor binding and activation. Several compounds containing ether and ester functionality were found to be potent agonists. Topical ocular administration of 5 , 18 , and 25 effectively reduced intra-ocular pressure in the hypertensive cynomolgus monkey eye in the range of 25–37%.