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Possible Drugs of the Future

Blase Deviant...

The reason most people say that they prefer heroin to fentanyl is not because of any subjective differences but because fentanyl [not the analogs] only lasts less than 2 hours as opposed to heroin's 4 to 6 hours. The rush is about the same as is the euphoria.
 
Anyone have any more information about Abbott laboratories' ABT-594? Or does anyone have any links to where I could find some info.?

Also, I definitely agree with blase deviant about the subjective effects being much more important than the potency...good example. Having that pointed out, regardless of potency, what possible future opioids have the most potential to produce euphoria similar, or better than, heroin? When it comes down to it, that's really what I'm looking for.
 
Re: Abott Laboratories' ABT-594 (from abott.com):

"Abbott scientists are currently researching ABT�594, an investigational compound for pain. The non-opioid, non-NSAID (Non-Steroidal Anti-Inflammatory) compound belongs to a new class of drugs called cholinergic channel modulators, which affect acetylcholine receptors to stop pain signals to the brain. Pre-clinical studies are promising, with ABT-594 exhibiting morphine-like efficacy."

Non-opioid? Most of the info. I've found (sources below) says it binds to nicotinic receptor(s), but I've yet to find any info. saying to has any effects on opiate receptors. Despite this, almost every article does make the comparison to morphine, suggesting it is anywhere between 50 to 200 times for potent (200x seems to be from the original poison from the frog, not the modified ABT-594).

More info./sources:
http://psa-rising.com/medicalpike/frog.htm
http://www.chemsoc.org/exemplarchem/entries/2004/icl_Pan/page5.html
http://www.azdr.com/articles/article1.html
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9729357&dopt=Abstract
(Most sources have basically the same information)
 
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I have a read a big fat document on this matter. This was up to date, referenced and posted some time last year. I only got it because my project supervisor handed us a copy. It is similar to nicotine, not morphine. Apparantly persons in a state of chronic pain are alot more likely to be smokers according to their statistics.
 
From joystick:

The only exciting, new, and probably addictive pain reliever being tested right now that I know of is Abbott laboratories' ABT-594 (chemically, 5-(2-azetidinylmethoxy)-2-chloropyridine. Not only is ABT-594 200x more potent than morphine as an analgesic in animal models, but it releases DA and NE (a la methamphetamine) and is a nicotinic receptor agonist (a la nicotine). Also, its action is not blocked by the co-administration of opiate antagonists such as naloxone or naltrexone. ABT-594 sounds promising, to say the least, in my opinion. Time will, hopefully, tell.
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He says it's "probably addictive." I thought he was implying that it was an opioid or acting on opioid receptors in one way or another. All the articles I've read suggest the exact opposite. Therefore Smyth, I agree with you...it does seem similar to nicotine, and not morphine...despite this, it could still prove to be a very effective pain reliever, and a non-addictive, non-opioid.
 
Wouldn't that be great? Anyone know if someone is doing any research into that area...preferably someone who is making that research public?
 
I was under the impression that QiHKAL, if it is ever published, will be about quinolamine alkaloids

On the subject of Abbott's new drug, it may not be an opioid, but it sounds damned addictive if you ask me. I say this not only because it's based off nicotine, which is itself quite addictive, but also because as far as I know, most drugs which are dopamine agonists, reuptake inhibitors, or increase the release of dopamine into the synapse are addictive. This is not to say that all dopaminergic drugs are addictive, but it seems that there is a definite trend.
 
QIHKAL is about isoquinoline alkaloids (if what I've read is correct). Isoquinolines are effectivly phenethylamines where the ethylamine side chain has been incorporated into a second ring, fused to the benzene nucleus

Technically, I suppose it should be called IIKHAL, but that looks like a bastard to pronounce!
 
I think "the simple plant isoquinolines" is just a intro for this one, as it's a bit removed from the phenethylamine and tryptamine drugs he's looked at in the past (no accumulated history of use, unlike the phenethylamines and tryptamines). This is the third of his trilogy (writers seem especially fond of trilogies, Tolkien had is for Lord of the Rings, and George Lucas is taking the piss with a trilogy of trilogies), and I think he's just laying the ground for the final tome.

Also, there's something that make me see him, sort of in the same way as the other two I mentioned (I actually think it's the insubordinate hair and beard - and his shirts!))
 
Sorry if the post seems random; I'm not a very good writer.

As for the piperidine ring in fentanyl, you can open it up at the 2-3 positions to make an open chain compound called "seco fentanyl"(1). It's 30x less potent than fentanyl and lasts half as long. There's lots of info on the web if you're looking for it. Not really appealing, but if one day they figure out how to lengthen the half like of the fentanyls, this could get interesting as it's not scheduled.
On another forum a long time ago someone found literature that found out if you add an ethyl bridge to fentanyls at the 2 and 6 position, the new compound retains activity, so possibly the open chain derivative will also be active.(2)
(3)and(4) are possible open chain derivatives of cocaine if broken at the same spot as fentanyl. I have no clue whether they are active.
 
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blase deviant said:
No offense, but all the carfentanyl stuff seems like dicksizing. IMO, it's not the potency, it's the subjective effects.

I'd rather take a 500mg of a drug if it gave me a better buzz as compared to a similar drug active at .00000005mg. Factoring in cost, etc...

E.x. heroin is less potent than fentanyl, but I've heard people say they don't like fentanyl.

Personally a drug I'd love to try but probably never will is levorphanol/levomethorphanol (I forget what the longer, pre-metabolization drug is called, but you all know what I mean).
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You miss the point, its not about what you want, what you like. Its what the people 'behind the scenes' want.

Drug users are like rats in somones house. They dont make the grocery list, they dont choose what is brought into the house, but their entire survival depends upon consuming what is brought in. Wether its top of the line blue cheese, or some kraft imitation cheese, you will eat it, for that is your survival.

But the owners, the people who bring the food, they will bring not what the rats want, but what they want, and they KNOW the rats will consume regardless, or they will die. Its leverage.

Super opioids will not appear because they are 'better high' than Heroin for the user, they will appear because they are better buisness for the dealer, for the trafficker, for the manufacturer, for the straight up money making and police avoidance.

The people at the top of the game dont care about you, what you want, what you like, wether you live or die, or anything inbetween. And they KNOW that no matter what, you, the rat, will always need to 'eat', regardless of how disgusting the food they bring in is.

Dealers are the puppetmasters of addicts. Whatever string they pull, you have no control but to carry out that movement. Its a beautiful thing, the symbiosis of the dealer/user relationship, on one side, is all the riches and power of the world, on the other side, is all the pain and despairity of the world.
 
^ Dude that's bullshit. Drug use is a market economy. Why do you think PCP is so hard to get? Because no one wants it. Yet MDMA is getting cheaper and cheaper in the US, because supply is increasing. People who know what they want don't buy crap cannabis. In my country, you can't get horrible cannabis, anywhere, no one would buy it, so no one sells it.

Furthermore, intellegent users can figure out ways to get drugs personally created for their needs.
 
Hi, I'm very interested in what fastandbulbous had to say about SAR's of opiates. Are there any particular articles you would suggest reading?
Also I was wondering whether or not it would be theoretically possible to design a compound with affinity for opioid receptors and activity reminiscent of the phenethylamine compounds (NE, DA, and 5-HT activity), possibly along the lines of a 3-phenyl-N-methyl-pyrrolidine?
(please forgive my probably horrible IUPAC nomenclature)
 
3-phenyl-N-methyl-pyrrolidine sounds interesting. I amnotsure that it would act at opioid receptors, butit might be an interesting psychostimulant--an analouge of phendimetrazine, methamphetamine and aminorex. Since it is technically an amphetamine, I bet it might release monoamines.
 
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