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%.
MeSH terms
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Animals
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Antihypertensive Agents / chemical synthesis
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Antihypertensive Agents / chemistry*
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Antihypertensive Agents / pharmacology*
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Benzofurans / chemical synthesis
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Benzofurans / chemistry*
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Benzofurans / pharmacology*
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Macaca fascicularis
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Muscle, Smooth, Vascular / cytology
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Muscle, Smooth, Vascular / drug effects
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Ocular Hypertension*
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Rats
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Receptor, Serotonin, 5-HT2A / chemistry
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Serotonin 5-HT2 Receptor Agonists*
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Serotonin Receptor Agonists / chemical synthesis
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Serotonin Receptor Agonists / chemistry*
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Serotonin Receptor Agonists / pharmacology*
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Structure-Activity Relationship
Substances
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Antihypertensive Agents
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Benzofurans
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Receptor, Serotonin, 5-HT2A
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Serotonin 5-HT2 Receptor Agonists
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Serotonin Receptor Agonists