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Old 11-10-2006, 00:39
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new sobering up drug.... invented in 1986 ?

browsing stuff tonight I stumbled upon references to a sobering up drug which was worked on in 1986, Ro15-4513.
looking into it, it seems that Roche was behind it and finally decided not to market it for ethical reasons.
I'm posting this because I remember people people talking about reversing the effects of alcohol here but cannot find the thread.

"Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-induced intoxication in the rat

PD Suzdak, SM Paul and JN Crawley


The ability of the imidazobenzodiazepine Ro15-4513 to antagonize the behavioral intoxication produced by ethanol and related short-chain alcohols was examined in the rat. Ro15-4513 dose dependently (0.5-10 mg/kg i.p.: IC50, 1.5 mg/kg) inhibited the intoxication induced by ethanol (2 g/kg), as well as t-amyl alcohol (0.36 g/kg) and methanol (4.66 g/kg). The effects of Ro15-4513 in blocking ethanol-induced intoxication were blocked by the benzodiazepine receptor antagonists Ro15-1788 and CGS-8216. However, Ro15-4513 was ineffective in antagonizing the intoxication observed after higher doses of ethanol (4 g/kg). In contrast, ethanol-induced intoxication was not antagonized by the benzodiazepine receptor antagonists Ro15-1788 (10 mg/kg) or CGS- 8216 (20 mg/kg), nor by the inverse agonists FG-7142 (10-30 mg/kg) or beta CCE (10 mg/kg). When administered after ethanol,Ro15-4513 also reversed ethanol-induced intoxication in a dose-dependent manner (2.5- 10 mg/kg i.p.: IC50, 5 mg/kg), an effect which was also blocked by Ro15- 1788 and CGS-8216. However, neither beta CCE (10 mg/kg) or FG-7142 (less than or equal to 30 mg/kg) alone reversed ethanol-induced intoxication. Moreover, beta CCE (10 mg/kg), when administered just before Ro15-4513, completely antagonized the actions of Ro15-4513 in reversing ethanol-induced intoxication. These data suggest that the ability of Ro15-4513 to antagonize, and to reverse, ethanol-induced intoxication is mediated via central benzodiazepine receptors"

i didn't remember this, and will look into it some more as I find this pretty fascinating. do any of you have more info on this 1986 breakthrough that seems to have been muffled or something ?
sorry if this is old news to many.
apparently the substance name was Ro15-4513

b

b

Reputation Comments on this post:
  
  Very interesting.
  
  almost revolutionary

Last edited by Jatelka; 08-06-2008 at 08:17. Reason: abstract included
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