Abstract
A series of conformationally restricted Gabapentin analogues has been synthesised. The pyrrolidine analogue (R)-2-Aza-spiro[4.5]decane-4-carboxylic acid hydrochloride (3a) had an IC50 of 120 nM, similar to that of Gabapentin (IC50 = 140 nM), at the Gabapentin binding site on the alpha2delta subunit of a calcium channel. Compound (3a) also reversed carrageenan induced hyperalgesia in rats.
MeSH terms
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Acetates / chemical synthesis
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Acetates / chemistry*
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Acetates / pharmacology
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Amines*
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Analgesics, Non-Narcotic / chemical synthesis
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Analgesics, Non-Narcotic / pharmacology
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Animals
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Convulsants / chemical synthesis
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Convulsants / pharmacology
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Cyclohexanecarboxylic Acids*
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Gabapentin
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Molecular Structure
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Rats
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gamma-Aminobutyric Acid*
Substances
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Acetates
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Amines
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Analgesics, Non-Narcotic
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Convulsants
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Cyclohexanecarboxylic Acids
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gamma-Aminobutyric Acid
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Gabapentin