Abstract
Desformylflustrabromine (dFBr; 1) and desformylflustrabromine-B (dFBr-B; 2) have been previously isolated from natural sources, and the former has been demonstrated to be a novel and selective positive allosteric modulator of alpha4beta2 nicotinic acetylcholine (nACh) receptors. The present study describes the synthesis of water-soluble salts of 1 and 2, and confirms and further investigates the actions of 1 and 2 using two-electrode voltage clamp recordings.
MeSH terms
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Allosteric Site
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Animals
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Bromine / chemistry*
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Chemistry, Pharmaceutical / methods
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Drug Design
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Humans
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Hydrocarbons, Brominated / chemical synthesis*
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Hydrocarbons, Brominated / pharmacology
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Indole Alkaloids / chemical synthesis*
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Indole Alkaloids / pharmacology
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Kinetics
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Magnetic Resonance Spectroscopy
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Nicotinic Antagonists / chemical synthesis*
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Nicotinic Antagonists / pharmacology
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Patch-Clamp Techniques
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Rats
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Receptors, Nicotinic / metabolism*
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Water / chemistry
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Xenopus
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alpha7 Nicotinic Acetylcholine Receptor
Substances
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Chrna7 protein, human
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Chrna7 protein, rat
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Hydrocarbons, Brominated
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Indole Alkaloids
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Nicotinic Antagonists
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Receptors, Nicotinic
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alpha7 Nicotinic Acetylcholine Receptor
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desformylflustrabromine
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nicotinic receptor alpha4beta2
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Water
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Bromine