The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin

…, S Bevan, G Bovermann, JJ Boelsterli…

Index: Walpole, Christopher S. J.; Bevan, Stuart; Bovermann, Guenter; Boelsterli, Johann J.; Breckenridge, Robin; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 13 p. 1942 - 1954

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Citation Number: 215

Abstract

Capsaicin and resiniferatoxin are natural products which act specifically on a subset of primary afferent sensory neurons to open a novel cation-selective ion channel in the plasma membrane. These sensory neurons are involved in nociception, and so, these agents are targets for the design of a novel class of analgesics. Although synthetic agonists at the capsaicin receptor have been described previously, competitive antagonists at this ...