Abstract
The iodobenzamide neuroleptic analogue (S)-N-(1-ethylpyrrolidin-2-ylmethyl)-2-hydroxy-5-iodo-6-methoxybenzamide (5-IBZM) was synthesized stereospecifically and its pharmacological properties were compared with the 3-iodo isomer (IBZM) used for imaging D(2) receptors in vivo. The isomer 5-IBZM had 100-fold lower affinity than IBZM and migrated with similar retention time as the byproduct formed during electrophilic iodination of BZM.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Benzamides / chemical synthesis*
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Benzamides / pharmacokinetics
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Indicators and Reagents
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Iodine Radioisotopes*
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Isotope Labeling / methods
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Molecular Structure
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / pharmacokinetics
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Structure-Activity Relationship
Substances
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Benzamides
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Indicators and Reagents
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Iodine Radioisotopes
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Pyrrolidines
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3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide