It is thought that Ro15-4513 antagonizes the effects of ethanol because the azido group at the 8- position of the benzene ring blocks the binding site for ethanol on the α4β3δ subtype of the GABA A receptor flumazenil, which has a fluorine at this position, does not block this binding site and so does not counteract the effects of ethanol. This meant that in contrast to flumazenil, which is ineffective at treating alcohol overdoses, Ro15-4513 showed potential as a useful alcohol antidote. Ro15-4513 was somewhat less effective than flumazenil at blocking the effects of benzodiazepines, but instead selectively blocked the effects of ethanol. Flumazenil effectively blocks the effects of benzodiazepine agonists such as alprazolam and diazepam and so is used for treating overdoses of these drugs but is ineffective in blocking alcohol actions. The main interest in Ro15-4513 was as an antidote to alcohol.
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