Talk:Ro15-4513

Chemical supply

This sounds like something I'd like to experiment with. Where can I acquire some? Miserlou 03:10, 6 November 2007 (UTC)

A doctor, or Roche Pharmaceutical. Wikipedia is not here to help you get drugs, sorry. --Astavats 22:19, 13 November 2007 (UTC)

Major rewrite

I think this article misses the whole point of why Ro15-4513 or any ligand with similar properties was never developed as a drug. To paraphrase a sentence from the current version of the article:

while Ro15-4513 is an effective antidote against moderate levels of alcohol intoxication, it might will be ineffective at treating life-threatening overdoses

With respect to antagonizing the effects of alcohol, Ro15-4513 only blocks the intoxicating effects of alcohol on higher CNS functions, but not the life threatening toxic effects. If an alcoholic took Ro15-4513, the alcoholic would likely continue to drink in search of a high but never reach it. This would lead to a high risk of death. To say that drug companies never developed such a drug for legal reasons is an understatement. It would be unethical to develop such a drug and if such a drug were developed, no regulatory authority that was functioning properly would ever approve it.

Therefore I feel that this article needs a major rewrite to emphasize that it would be unethical to develop such a drug. Boghog2 (talk) 20:22, 9 April 2008 (UTC)

This is a good point, but interest in potential alcohol antidotes isn't limited to treatment of life-threatening acute overdose. If you read some of the review articles discussing this compound they mention that another application could be counteracting the effects of moderate alcohol consumption (which Ro15-4513 does quite well). This is because there are a lot of social situations where people come under strong pressure to drink alcohol, and non-drinkers may be disadvantaged - for instance where a company has a culture of "work drinks" a non-drinker may be felt to be "not part of the team" and potentially miss out on opportunities for promotion or pay rises due to their reluctance to drink. For this kind of situation an alcohol antidote could be quite useful so that someone could take part in social drinking but without actually becoming intoxicated.

However one of the concerns about this is that a person might then feel sober despite having had several drinks and go to drive home, only to have the shorter acting Ro15-4513 wear off before the alcohol and cause them to become drunk while they were behind the wheel. The other concern is of course as you say that it would not be effective at treating serious overdoses, but even so given the multiple actions of alcohol you would probably need a mix of drugs to be an effective antidote, and a longer-acting version of Ro15-4513 could be a useful component of such a formulation, alongside other drugs to counteract the effects of alcohol at NMDA receptors, sodium channels etc. Meodipt (talk) 09:00, 13 April 2008 (UTC)

OK, I may have over simplified things a bit. I need to go back and re-read some of this literature. Ultimately it may be very difficult to determine why Roche did not develop an alcohol antagonizing drug or even what indication Roche was pursuing when Ro15-4513 was discovered. The precise reasons why drug companies start or stop research projects is often not disclosed because of competitive concerns. Cheers. Boghog2 (talk) 09:22, 13 April 2008 (UTC)

Research

I think the possibilities of using Ro15-4513 as a drug to counteract the effects of alcohol use are no longer the concern of most that use it. Its use as a precursor/template for other drugs aside, the anti-alcohol effects are fading into history and as they do, this article grows out of date. Although the search for a drug that can effectively remove the side-effects of alcohol use is still on, and indeed the addictive and dangerous effects, Ro15-4513 is being pushed forward as an investigative ligand for GABA research. The finer mechanisms of GABAergic transmission, especially concerning the less common receptor subtypes in the limbic system and cortex, are still the subjects of major debate, and ligands selective for different subtypes are helping to pin down the functions of the different receptors, both at the synapse and holistically, as players in emotional control, impulse control or, importantly, vulnerability to addictive behaviour. Bluefloyd1 (talk) 10:08, 24 April 2008 (UTC)

RO15-4513 is a complex mixed action drug. Depending on the receptor subtype of GABAA, it can function as an partial agonist, partial inverse agonist, or neutral antagonist. It may be misleading to introduce the drug as a weak partial inverse agonist of diazepam sensitive GABAA receptors. — Preceding unsigned comment added by AstarothN (talk • contribs) 17:08, 4 June 2014 (UTC)

This is a complex drug

RO15-4513 is a complex mixed action drug. Depending on the receptor subtype of GABAA, it can function as an partial agonist, partial inverse agonist, or neutral antagonist. It may be misleading to introduce the drug as a weak partial inverse agonist of diazepam sensitive GABAA receptors. — Preceding unsigned comment added by AstarothN (talk • contribs) 17:11, 4 June 2014 (UTC)

In which case, if you can cite that claim then perhaps write it as you have here? Testem (talk) 09:54, 6 June 2014 (UTC)