Abstract
Radioreceptor analysis showed that human beta-casomorphin-7 displaced 3H-spiperone from 5-HT2-serotonin receptors of the rat cerebral frontal cortex: EC50 8 +/- 1 microM. Human and bovine beta-casomorphin-7 dose-dependently blocked serotonin-induced human platelet aggregation: IC50 5 +/- 1 and 20 +/- 4 microM, respectively. It was proved that beta-casomorphins-7 act as 5-HT2-serotonin receptor antagonists; one of the mechanisms of their biological effects is presumably associated with modulation of the serotoninergic system.
MeSH terms
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Animals
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Cattle
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Cerebral Cortex / drug effects
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Dopamine Antagonists / pharmacology
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Dose-Response Relationship, Drug
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Endorphins / metabolism*
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Humans
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Inhibitory Concentration 50
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Ketanserin / pharmacology
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Peptide Fragments / metabolism*
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Platelet Aggregation
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Protein Binding
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Rats
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Receptors, Serotonin, 5-HT2 / metabolism*
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Serotonin Antagonists / pharmacology
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Spiperone / pharmacology
Substances
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Dopamine Antagonists
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Endorphins
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Peptide Fragments
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Receptors, Serotonin, 5-HT2
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Serotonin Antagonists
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Spiperone
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beta-casomorphin 7
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Ketanserin