Abstract
SR 48968 was first described as a NK-2 nonpeptide receptor antagonist; we report here that SR 48968 interacts also with guinea pig but not rat NK-3 cortical binding sites. Furthermore, SR 48968 is shown to inhibit the senktide- (a NK-3 selective agonist) evoked stimulation of phosphoinositide turnover in guinea pig ileum slices. The species difference observed for the NK-3 receptor with SR 48968 was confirmed by the determination of the affinities of NK-3 peptide agonists. [Pro7]neurokinin B particularly was found to have a greater affinity for cortical NK-3 binding sites in the rat than in the guinea pig.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzamides / pharmacology*
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Binding, Competitive
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Cell Membrane / metabolism
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Cerebral Cortex / metabolism*
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Enzyme Activation
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Guinea Pigs
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Ileum / metabolism*
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In Vitro Techniques
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Kinetics
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Male
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Muscle, Smooth / metabolism*
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Neurokinin A / antagonists & inhibitors*
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Peptide Fragments / metabolism
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Peptide Fragments / pharmacology
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Phosphatidylinositols / metabolism*
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Piperidines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Neurotransmitter / antagonists & inhibitors*
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Receptors, Tachykinin
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Substance P / analogs & derivatives
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Substance P / metabolism
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Substance P / pharmacology
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Synaptosomes / metabolism*
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Tachykinins / pharmacology
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Type C Phospholipases / metabolism*
Substances
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Benzamides
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Peptide Fragments
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Phosphatidylinositols
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Piperidines
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Receptors, Neurotransmitter
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Receptors, Tachykinin
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Tachykinins
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senktide
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Substance P
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SR 48968
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Neurokinin A
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Type C Phospholipases