Abstract
Analogues of pindolol, 1-(1H-indol-4-yloxy)-3-isopropylamino-propan-2-ol, were synthesized and evaluated as 5-HT(1A) receptor antagonists. The structural features required for optimal binding to the 5-HT1A receptor are as follows: S-2-propanol linker, 4-indoloxy substituent, and a large lipophilic cyclic amine substituent.
MeSH terms
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Animals
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Corticosterone / blood
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Hydroxylation
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Indoles / chemistry*
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Isomerism
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Male
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Molecular Structure
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Oxidation-Reduction
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Propanolamines / chemical synthesis
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Propanolamines / chemistry*
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Propanolamines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptor, Serotonin, 5-HT1A / metabolism*
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Serotonin 5-HT1 Receptor Antagonists*
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Structure-Activity Relationship
Substances
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Indoles
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Propanolamines
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Serotonin 5-HT1 Receptor Antagonists
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Receptor, Serotonin, 5-HT1A
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Corticosterone