Abstract
Although bombesin (BN) and substance P share only the C-terminal dipeptide amide, some substance P receptor antagonists are also weak bombesin receptor antagonists. In order to increase the selectivity of the antagonism for the BN receptor, a series of hybrid peptides were synthesized by the solid-phase methodology, and screened on 3T3 fibroblasts for binding and mitogenic activity. The analogues inhibiting BN-induced thymidine incorporation were further tested for peripheral (amylase release and urinary bladder contraction) and central activity (grooming behaviour).
MeSH terms
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3T3 Cells
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Amino Acid Sequence
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Amylases / metabolism
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Animals
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Grooming / drug effects
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In Vitro Techniques
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Male
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Mice
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Mitogens / pharmacology
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Molecular Sequence Data
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Pancreas / drug effects
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Pancreas / enzymology
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Rats
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Receptors, Bombesin
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Receptors, Neurokinin-1
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Receptors, Neurotransmitter / antagonists & inhibitors*
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Substance P / antagonists & inhibitors*
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Urinary Bladder / drug effects
Substances
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Mitogens
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Receptors, Bombesin
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Receptors, Neurokinin-1
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Receptors, Neurotransmitter
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Substance P
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Amylases