exotic opioids (pics)

[jdfc]

Mad Scientist, you have any leads for me to pursue regarding the Meperidine analogs?? Like do you have the names for the ones youve seen with these mu-agonist and DRI pharmacologic profiles but are lower dose than mep?? One in the MCG range is my dream. You find it and ill tell you if its any good.

And just for the record, LSD also is a mu-agonist and ALOT of other shit, and its also active at a very low dosage range...

 

[mad_scientist]

Mad Scientist, you have any leads for me to pursue regarding the Meperidine analogs?? Like do you have the names for the ones youve seen with these mu-agonist and DRI pharmacologic profiles but are lower dose than mep?? One in the MCG range is my dream. You find it and ill tell you if its any good.

Stacey A. Lomenzo, Jill B. Rhoden, Sari Izenwasser, Dean Wade, Theresa Kopajtic, Jonathan L. Katz, and Mark L. Trudell. Synthesis and Biological Evaluation of Meperidine Analogues at Monoamine Transporters. J. Med. Chem.; 2005; 48 (5): 1336-1343

Abstract:

A series of aryl-substituted meperidine analogues was synthesized, and the binding affinities were determined at the DAT, SERT, and NET as well as at mu-opioid receptors. Generally the analogues exhibited increased affinity for the DAT and SERT relative to meperidine but exhibited low binding affinity for the NET. The 2-naphthyl derivative 7f was the most potent ligand at the SERT (Ki = 0.0072 M) and was the most selective ligand for the SERT over the DAT (DAT/SERT = 158 ) and mu-opioid receptors (/SERT = 281). The 3,4-dichlorophenyl derivative 7e was the most potent ligand at the DAT (Ki = 0.125 M) and was the most selective ligand for the DAT over mu-opioid receptors (/DAT = 16.3) but remained slightly more selective for the SERT over the DAT(DAT/SERT = 6.68 ). Three compounds, the 3,4-dichlorophenyl derivative 7e and the 2-naphthyl analogues 6f and 7f, were identified that were more potent at the DAT than meperidine and that exhibited well-defined biphasic dopamine uptake inhibition similar to meperidine. However, none of the analogues tested produced locomotor effects or substituted for cocaine in drug discrimination studies, suggesting that the mu-opioid effects of these analogues may contribute to the poor efficacy observed in vivo.

 

[dbailey11]

Ever heard of Ziconotide? It comes from the venom of the marine cone shell snail, and is said to be a 1000 times more potent than morphine with no side effects such as addiction and withdrawl. It's already being used in clinical trials with cancer and AIDS patients who don't respond to traditional opiate painkillers like morphine. Sounds really interesting and makes me wonder at all the as yet udiscovered natural chemicals out there. Maybe there's a natural hallucinogen out there somewhere that could blow away anything we've ever seen so far. The possibilities are astounding really.

 

[jdfc]

Stacey A. Lomenzo, Jill B. Rhoden, Sari Izenwasser, Dean Wade, Theresa Kopajtic, Jonathan L. Katz, and Mark L. Trudell. Synthesis and Biological Evaluation of Meperidine Analogues at Monoamine Transporters. J. Med. Chem.; 2005; 48 (5): 1336-1343

Abstract:

A series of aryl-substituted meperidine analogues was synthesized, and the binding affinities were determined at the DAT, SERT, and NET as well as at mu-opioid receptors. Generally the analogues exhibited increased affinity for the DAT and SERT relative to meperidine but exhibited low binding affinity for the NET. The 2-naphthyl derivative 7f was the most potent ligand at the SERT (Ki = 0.0072 M) and was the most selective ligand for the SERT over the DAT (DAT/SERT = 158 ) and mu-opioid receptors (/SERT = 281). The 3,4-dichlorophenyl derivative 7e was the most potent ligand at the DAT (Ki = 0.125 M) and was the most selective ligand for the DAT over mu-opioid receptors (/DAT = 16.3) but remained slightly more selective for the SERT over the DAT(DAT/SERT = 6.68 ). Three compounds, the 3,4-dichlorophenyl derivative 7e and the 2-naphthyl analogues 6f and 7f, were identified that were more potent at the DAT than meperidine and that exhibited well-defined biphasic dopamine uptake inhibition similar to meperidine. However, none of the analogues tested produced locomotor effects or substituted for cocaine in drug discrimination studies, suggesting that the mu-opioid effects of these analogues may contribute to the poor efficacy observed in vivo.

I dont suppose you have the DAT/SERT/Mu1/2 Ki and affinity values for Meperidine tucked back in your closet there do you? thatd be a nice peice of information right about... now.

And in these guys conclusion, I dont see them comparing the Mu1 agonist Ki potency values for Meperidine vs. 7e, 6f and 7f, maybe its in the full article *dont suppose you got that?*, but any clue if these derivs have lower Ki values as Mu1-agonists vs. Meperidine?? Because I dont see anywhere in this abstract stating theyre stronger than Meperidine as an opioid, id hope thats in the full article.

 

[johanneschimpo]

I'm drunk but I just wanted to state that the molecular structures for meperdine and methylphenidate are shockingly similar.
I guess that explains the effects on dopamine in addition to its role as an opioid?

 

[weephar]

Wow, very interesting...any idea how the strength of these compare to morphine? Or, are these just opiods that were synthed in a lab and documented but never really tested/used? Are there chemists trying to bring these to the market (white or black?)? Finally, wouldn't the US Analog Act make these illegal here(obviously not in other countries)?

 

[haribo1]

Ever heard of Ziconotide? It comes from the venom of the marine cone shell snail, and is said to be a 1000 times more potent than morphine with no side effects such as addiction and withdrawl. It's already being used in clinical trials with cancer and AIDS patients who don't respond to traditional opiate painkillers like morphine. Sounds really interesting and makes me wonder at all the as yet udiscovered natural chemicals out there. Maybe there's a natural hallucinogen out there somewhere that could blow away anything we've ever seen so far. The possibilities are astounding really.

Not an opiate. Doesn't work on opiate receptors.

 

[jdfc]

1) any idea how the strength of these compare to morphine?
(2) Or, are these just opiods that were synthed in a lab and documented but never really tested/used?
(3) Are there chemists trying to bring these to the market (white or black?)?
(4) Finally, wouldn't the US Analog Act make these illegal here(obviously not in other countries)?

1) im trying to figure the same thing, without Mu1 Ki values for Meperidine and these analogs thats pretty hard to figure

2) seems theyve been decently documented if there is SERT/DAT/NET affinity profiles and opioidergic data collected

3) most compounds ever synthed are synthed simply to study structure activity relationships and rarely do any of these compounds ever end up in legal use, thus most any analogs you see will only be received on the blackmarket

4) it doesnt matter if the chemical you make is a methyl group away from a sched 1 or is a brand new chemical, you WILL BE CHARGED REGARDLESS, they dont give a shit about the chemical differences what the analog act really does is stop ANY chemical, new, old, or analog that anyone would ever make IF they ever sell that chemical, discuss that chemical, use that chemical, or market that chemical as an alternative to any scheduled chemical, PERIOD. However the BENEFIT of designer drugs is that the chance for identification is 1/100 on the STREET level.

Example; you whip up some hip new Meperidine analog and its passed off as heroin. One of the suppliers gets raided by police, they seize 200g of this heroin mimic material. Step to survival: He DENIES this powder being any drug of any kind. Immediately police are required by law to test the substance once the suspect denies its illegality. It will produce a negative result on the test, they WILL use street side drug test kits, if they claim theyre taking it back to the lab it only means theyre going to run the same street side drug test kits just back at the station (beleive me!). It ends here. Their investigation is inconclusive, and the charges are dropped. Further identification of the material is very-VERY slim, and would only occur in very large quantities of an unknown suspected drug. What you see in the DEA microgram are a very very very very very very small fraction of local-level law enforcement unidentified seized materials sent in. Very rarely is this done, mainly only involving items that are blatantly drug-related but unidentifiable (blotters that dont test as LSD, tablets, etc)

The MOMENT the drug inside that mimic-heroin were detected, it doesnt matter AT ALL what "analog" chemical it is, your going to be charged, I guarantee. Sorry I have to lecture on this, cause people here act like theyre actually safe by avoiding the analog act... your not. If police want you fucked over, your going to get fucked over.

 

[vecktor]

^ fortunately the US is not the only country in the world.

and even in the US the track record of using the analog act is patchy, there have been very few prosecutions using it, and the DEA has resorted to scheduling things to prevent the vagaries associated with the analog act.

I would also think that they would use GC-MS HPLC-MS to identify things, a test kit result would not stand up in court as an identification, I suppose it does depend on whether it is the DEA or Billy Bob from the local Loserville sheriffs office who busts you, I don't know, I'm not American and I find America baffling.

 

[dbailey11]

Not an opiate. Doesn't work on opiate receptors.

Yeah but tell me that isn't interesting. The fact that it kills pain and has no effect on opiate receptors is very noteworthy to me. I just wonder how it feels. If it's euphoric with no potential for addiction that would really be something.

 

[LuxEtVeritas]

pretty sure there is no euphoria whatsoever

 

[hussness]

Ziconotide is an N-type calcium channel blocker. The pharmacological mechanism isn't related to opioid receptor agonism. It doesn't really produce euphoria, and requires intrathecal administration. Not really worth it if you're looking to get high.