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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.

Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors. Their ester prodrugs 6 and 8 were orally active in three models of pain: reversal of formalin-induced paw licking, carrageenan-induced thermal hyperalgesia, and capsaicin-induced mechanical hyperalgesia.[1]

References

  1. Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. Dominguez, E., Iyengar, S., Shannon, H.E., Bleakman, D., Alt, A., Arnold, B.M., Bell, M.G., Bleisch, T.J., Buckmaster, J.L., Castano, A.M., Del Prado, M., Escribano, A., Filla, S.A., Ho, K.H., Hudziak, K.J., Jones, C.K., Martinez-Perez, J.A., Mateo, A., Mathes, B.M., Mattiuz, E.L., Ogden, A.M., Simmons, R.M., Stack, D.R., Stratford, R.E., Winter, M.A., Wu, Z., Ornstein, P.L. J. Med. Chem. (2005) [Pubmed]
 
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