Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity |
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| Authors: | Feng Zixia Mohapatra Suchismita Klimko Peter G Hellberg Mark R May Jesse A Kelly Curtis Williams Gary McLaughlin Marsha A Sharif Najam A |
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| Affiliation: | Alcon Research, Ltd, Research Chemistry, 6201 South Freeway, Fort Worth, TX 76134, USA. |
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| 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%. |
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