Abstract
A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.
MeSH terms
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Administration, Oral
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Animals
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Benzamidines / chemical synthesis
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Benzamidines / pharmacology*
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Carrageenan
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Drug Evaluation, Preclinical
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Hyperalgesia / drug therapy
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Pain / drug therapy
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Psychomotor Performance / drug effects
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Rats
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Benzamidines
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NR2B NMDA receptor
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Receptors, N-Methyl-D-Aspartate
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Carrageenan