Abstract
Using synthetic N-terminal fragments of galanin, galanin (1-7), galanin (1-9), galanin (1-12) and galanin (1-16), we have shown that the minimal sequence required for inhibition of acetylcholine release in vivo from rat ventral hippocampus corresponds to galanin (1-12). The fragment (1-9) displays activity in vivo but only at a very high concentration of 6.23 nmol while galanin (1-7) and C-terminal fragment (17-29) are without effect. Binding studies showed that galanin (1-16) and galanin (1-12) bind with submicromolar IC50 values to rat hippocampal galanin receptors. Galanin (1-9) has substantially lower affinity towards rat ventral hippocampal galanin receptor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholine / metabolism*
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Animals
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Binding, Competitive / drug effects
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Galanin
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Hippocampus / drug effects
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Hippocampus / metabolism*
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In Vitro Techniques
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Ligands
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Male
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Membranes / drug effects
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Membranes / metabolism
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Neuropeptides / pharmacology*
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Peptide Fragments / pharmacology*
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Peptides / pharmacology*
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Rats
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Rats, Inbred Strains
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Rats, Sprague-Dawley
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Receptors, Galanin
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Receptors, Gastrointestinal Hormone / drug effects
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Receptors, Gastrointestinal Hormone / metabolism
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Scopolamine / antagonists & inhibitors
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Scopolamine / pharmacology
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Structure-Activity Relationship
Substances
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Ligands
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Neuropeptides
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Peptide Fragments
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Peptides
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Receptors, Galanin
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Receptors, Gastrointestinal Hormone
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Galanin
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Scopolamine
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Acetylcholine