Abstract
A range of 3-alkylated five-membered ring derivatives of Gabapentin were synthesized and several were found to have good levels of potency against the alpha2delta calcium subunit of a voltage-gated calcium channel. Two compounds were profiled in in vivo models of pain and anxiety.
Copyright 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Amines / chemical synthesis*
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Amines / chemistry
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Amines / pharmacology
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Amino Acids / chemical synthesis*
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Amino Acids / chemistry
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Amino Acids / pharmacology
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Animals
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Anti-Anxiety Agents / chemical synthesis*
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Anti-Anxiety Agents / chemistry
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Anti-Anxiety Agents / pharmacology
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Calcium Channels / metabolism
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Carrageenan / pharmacology
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Cyclohexanecarboxylic Acids / chemical synthesis*
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Cyclohexanecarboxylic Acids / chemistry
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Cyclohexanecarboxylic Acids / pharmacology
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Cyclopentanes / chemical synthesis*
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Cyclopentanes / chemistry
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Cyclopentanes / pharmacology
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Gabapentin
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Hyperalgesia / chemically induced
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Hyperalgesia / drug therapy
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Rats
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Stereoisomerism
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gamma-Aminobutyric Acid / chemical synthesis*
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gamma-Aminobutyric Acid / chemistry
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gamma-Aminobutyric Acid / pharmacology
Substances
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Amines
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Amino Acids
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Anti-Anxiety Agents
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Calcium Channels
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Cyclohexanecarboxylic Acids
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Cyclopentanes
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gamma-Aminobutyric Acid
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Gabapentin
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Carrageenan