Abstract
A series of 2-amino and 2-methoxy quinoline-6-carboxamide derivatives have been synthesized and their metabotropic glutamate receptor type 1 (mGluR1) antagonistic activities were evaluated in a functional cell-based assay. The compound 13c showed the highest potency with IC50 value of 2.16 µM against mGluR1. Finally, in vivo evaluation of 13c in the rat spinal nerve ligation (SNL) model exhibited weak analgesic effects with regard to both mechanical allodynia and cold allodynia.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cold Temperature
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Dose-Response Relationship, Drug
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
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Humans
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Hyperalgesia / drug therapy
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Mice
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Molecular Structure
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Neuralgia / drug therapy*
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Pain Measurement / drug effects
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Piperidines / pharmacology*
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Quinolines / chemical synthesis
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Quinolines / chemistry
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Quinolines / pharmacology*
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Rats
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Ether-A-Go-Go Potassium Channels
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N-ethyl-2-(piperidin-1-yl)quinoline-6-carboxamide
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Piperidines
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Quinolines
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor type 1