Abstract
A series of cyclic pseudopeptides were synthesized containing the sequence -Trp-Phe-(D)-PhePsiCH2NH-, the terminal ends of which were bound to 2-carboxy succinate or enantiomerically enriched tricarballylic acid to give the final cyclic structures. These two molecules and their subsequent derivatives were screened for h-NK2 receptor binding and functional antagonist activity on the rabbit urinary bladder.
MeSH terms
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Animals
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Cyclization
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Molecular Mimicry
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Oligopeptides / chemical synthesis
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Oligopeptides / pharmacology
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / pharmacology
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Rabbits
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Radioligand Assay
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Receptors, Neurokinin-2 / antagonists & inhibitors*
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Structure-Activity Relationship
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Succinic Acid / chemistry
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Tricarboxylic Acids / chemistry
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Urinary Bladder / drug effects
Substances
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Oligopeptides
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Peptides, Cyclic
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Receptors, Neurokinin-2
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Tricarboxylic Acids
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Succinic Acid
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tricarballylic acid