Drug info - new sobering up drug.... invented in 1986 ?

Discussion in 'Alcohol' started by Benga, Oct 11, 2006.

  1. Benga

    Benga Platinum Member & Advisor

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    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
     
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  2. Benga

    Benga Platinum Member & Advisor

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    Re: Ro15-4513 alcohol effect reversion...new sobering up drug.... invented in 1986 ?

    not going anywhere trying to dig this one up online.
    no one remembers this from 20 years ago ?
    don't know, maybe i'm stuck in a rut but the existence of a substance designed to breakdown / reverse effects of alcohol is definetly news to me ! and interesting news at that, for various reasons !
    i'd really like to know more on this story, Roche's Ro15-4513 ...
    what happened ?

    b
     
  3. Benga

    Benga Platinum Member & Advisor

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    apparently this was worked on as a treatment for alcohol addiction rather than as a way of reversing alcohol effects in case emergency sobriety was needed. this makes more sense as to why it had less potential.
    yet i find it hard to believe research on a substance reversing effects of alcohol quickly hasn't been worked on more, i see many practical uses, and actually something the military / strategic lines of work might be interested in as well, or maybe i've just been exposed to too many Vietnam movies where the partying boys are suddenly ambushed.