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N&PD Moderators: Skorpio | thegreenhand
Mephedrone Versions
- Thread starter Doclad
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Limpet_Chicken
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I read the thread on it. Vendors selling 'stuff' that was said by them to be ten percent RH-34 and the rest of it creatine.
Can't go from something like that. Also, one failure does not an entire class garbage make. IF it is a failure. Also a lot of bomamine-panic due to the 2-MeO-benzylamino group. This isn't on an amphetamine, or phenethylamine, cathinone. Its on ketanserin which has been disembowelled. Not WHOLLY dissimilar to tryptamines structurally in terms of things like the orientation of the nitrogens. I don't see reason for 'bomamine panic' when the same group has been grafted onto an entirely new backbone. That'd be like say, expecting 5-MeO-LSD to be more potent because 5-MeO-DMT is compared to DMT. Thats a closer skeleton by far. This is an entirely new entity.
And just imagine if Shulgin had only done oral trials of DMT, or if the first one he synthesized was say, 5-MeO-PYr-T. The latter sounds more poisonous and miserable than drug-worthy. If he'd shitcanned every tryptamine because of the one, then it would have been throwing hundreds of babies out with 1ml of bath water.
That 2-MeO-benzyl group has a phenyl ring which can have all manner of mono, di, tri, tetrasubstitutions done to it, the benzylic carbon could be modified with a substituent, the quinazolinedione group could be tweaked, one keto group removed, both, all manner of things done to it too. Just think, one single failure, if RH-34 is, doesn't mean we can't bastardize ketanserin to the point its speaking american english in tongues interspersed with strings of profanity in aramaic, and something good can come out of it.
Any reports based on a shady fucker flogging claimed 10% RH-34 in 90% creatine, thats not worthy of denouncing a single substance never mind a whole hitherto unexplored backbone.
Can't go from something like that. Also, one failure does not an entire class garbage make. IF it is a failure. Also a lot of bomamine-panic due to the 2-MeO-benzylamino group. This isn't on an amphetamine, or phenethylamine, cathinone. Its on ketanserin which has been disembowelled. Not WHOLLY dissimilar to tryptamines structurally in terms of things like the orientation of the nitrogens. I don't see reason for 'bomamine panic' when the same group has been grafted onto an entirely new backbone. That'd be like say, expecting 5-MeO-LSD to be more potent because 5-MeO-DMT is compared to DMT. Thats a closer skeleton by far. This is an entirely new entity.
And just imagine if Shulgin had only done oral trials of DMT, or if the first one he synthesized was say, 5-MeO-PYr-T. The latter sounds more poisonous and miserable than drug-worthy. If he'd shitcanned every tryptamine because of the one, then it would have been throwing hundreds of babies out with 1ml of bath water.
That 2-MeO-benzyl group has a phenyl ring which can have all manner of mono, di, tri, tetrasubstitutions done to it, the benzylic carbon could be modified with a substituent, the quinazolinedione group could be tweaked, one keto group removed, both, all manner of things done to it too. Just think, one single failure, if RH-34 is, doesn't mean we can't bastardize ketanserin to the point its speaking american english in tongues interspersed with strings of profanity in aramaic, and something good can come out of it.
Any reports based on a shady fucker flogging claimed 10% RH-34 in 90% creatine, thats not worthy of denouncing a single substance never mind a whole hitherto unexplored backbone.
swedger77
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QUALTIY statement! :D
Oxidation of (pseudo)ephedrine was popular in Russia and the US in the 1990s. Ring-substitution of the 3-carbon β-ketones has not been widely explored. for the 2-carbon (bk-2Cx and so on) produced a few good (but too costly to make) products. I had the misfortune to try bk-mescaline and when I reached 1g, I just threw up. Now βk-proscaline WAS good and the unexpected aspect was that that the terminal carbon of the n-propoxy moiety was oxidized rendering it safer than most of the class. The thioethers were NEVER tried. The potential MAOI activity put the designer off. I've often wondered if the S in 2-CT-7 is oxidized and that was the species responsible for MAOI activity.
As a class, the β-ketones do not appear to have any special activity making them worthy of further research but I'm hoping someone (Sekio, Adder, Limpet Chicken, I'm pointing at you) has looked into the activity of (S)-βk-DON or indeed (S)-βk-MDON (Moon). Now I accept I'm always the one shaking my head at aromatic nitro groups and EP0634999A1 paints a bleak picture for p-nitro amphetamine but with the o-methoxy present, I don't think it will interact in such a manner. Clearly it has much lower affinity for the 5HT-2a receptors but it's LogP (especially with the N-methyl) & pKa look OK and oxidation of the α-methyl becomes the metabolic pathway (dimerization suppressed by N-methyl simplifying study of metabolism). Why the βk you may ask, well because 4 liver enzymes appear able to perform said oxidation (2 form the aldehyde, 1 oxidizes the aldehyde and 1 goes from alkyl to carboxylic acid directly) and the fact that compared with the parent compound, it circulates the body offering the chance for said enzymes do their work.
It seems that few people have studied the enantiomers of chiral hallucinogens/entactogen. Some years ago we had samples of AMT optically resolved on the basis that the (2R) isomer overlays LSD and that the team at Upjohn who researched AET (Monase) & 7-methyl AET discovered that it was the 2S isomers were the more potent reuptake inhibitors. AMT was apparently used as an antidepressant in Russia (Indopan), the basis of their work. Well, the MAOI activities was worryingly high but like ketamine, the optical isomers of AMT display strikingly different properties. Of the series, 7,N,N-TMT proved to be DMT+ since both the affinity and cLogP were higher & the pKa was more amenable. Sadly, it costs a fortune to make due to the 7-methyl-1H-indole-3-carbaldehyde.
To end on a more positive note, while a 7-methyl didn't inhibit 5HT-2a affinity, larger groups do. I suggest that 7-bromo, 7-trifluoromethyl, 7-nitrile & 7-nitro will be entactogens and optical resolution with the unwanted enantiomer oxidized back to the ketone and fed back into the feed might be a good and safe MD(M)A alternative (depending on laws on your locale). I would certainly be interested to know if the nitro is safe because if it is, it is a convenient way for your body to metabolize it lowering duration. I don't know about anyone else but one of the key things about MDMA is it's duration. 4 hours is enough and while my wife initially loved a novel alternative I researched, at about hour 8 she began flagging and at hour 12 had to take some diazepam to stop the muscular pain but couldn't sleep until 16 hours had elapsed. That was p-TFM aminorex. The problems were solved but then the law changed and even people who make a hobby from rational design of novel psychoactives can find themselves in serious trouble.
That wasn't positive was it? Well, OK, so novel steroids are an open field and Daniel Lednicer has written a wonderful book on the subject. My signed copy has the words 'this book is dedicated to the libido, without which this book would neither be necessary nor possible'. The only 2 people I grew up idolizing are still with us, Daniel Lednicer and David Nichols. Both have encouraged me, discussed serious research, lab-culture and tittle tattle with me and both have placed my safety as a matter they are concerned about. Please don't bombard them with vacuous communications but if you discover a novel compound within their realms of expertize then they really are interested. Even Derek P. Reynolds (he who designed isotilidine) was interested to know that a 2-step synthesis was possible based on a 2016 paper. I'm nobody special but I am polite and I am courteous and as I get older, youngsters do contact me for information and while I am flattered, it is their education and helping them become better than me is my goal. In short - I always want to be the most stupid person in the room; that way I have the most to learn from others.
As a class, the β-ketones do not appear to have any special activity making them worthy of further research but I'm hoping someone (Sekio, Adder, Limpet Chicken, I'm pointing at you) has looked into the activity of (S)-βk-DON or indeed (S)-βk-MDON (Moon). Now I accept I'm always the one shaking my head at aromatic nitro groups and EP0634999A1 paints a bleak picture for p-nitro amphetamine but with the o-methoxy present, I don't think it will interact in such a manner. Clearly it has much lower affinity for the 5HT-2a receptors but it's LogP (especially with the N-methyl) & pKa look OK and oxidation of the α-methyl becomes the metabolic pathway (dimerization suppressed by N-methyl simplifying study of metabolism). Why the βk you may ask, well because 4 liver enzymes appear able to perform said oxidation (2 form the aldehyde, 1 oxidizes the aldehyde and 1 goes from alkyl to carboxylic acid directly) and the fact that compared with the parent compound, it circulates the body offering the chance for said enzymes do their work.
It seems that few people have studied the enantiomers of chiral hallucinogens/entactogen. Some years ago we had samples of AMT optically resolved on the basis that the (2R) isomer overlays LSD and that the team at Upjohn who researched AET (Monase) & 7-methyl AET discovered that it was the 2S isomers were the more potent reuptake inhibitors. AMT was apparently used as an antidepressant in Russia (Indopan), the basis of their work. Well, the MAOI activities was worryingly high but like ketamine, the optical isomers of AMT display strikingly different properties. Of the series, 7,N,N-TMT proved to be DMT+ since both the affinity and cLogP were higher & the pKa was more amenable. Sadly, it costs a fortune to make due to the 7-methyl-1H-indole-3-carbaldehyde.
To end on a more positive note, while a 7-methyl didn't inhibit 5HT-2a affinity, larger groups do. I suggest that 7-bromo, 7-trifluoromethyl, 7-nitrile & 7-nitro will be entactogens and optical resolution with the unwanted enantiomer oxidized back to the ketone and fed back into the feed might be a good and safe MD(M)A alternative (depending on laws on your locale). I would certainly be interested to know if the nitro is safe because if it is, it is a convenient way for your body to metabolize it lowering duration. I don't know about anyone else but one of the key things about MDMA is it's duration. 4 hours is enough and while my wife initially loved a novel alternative I researched, at about hour 8 she began flagging and at hour 12 had to take some diazepam to stop the muscular pain but couldn't sleep until 16 hours had elapsed. That was p-TFM aminorex. The problems were solved but then the law changed and even people who make a hobby from rational design of novel psychoactives can find themselves in serious trouble.
That wasn't positive was it? Well, OK, so novel steroids are an open field and Daniel Lednicer has written a wonderful book on the subject. My signed copy has the words 'this book is dedicated to the libido, without which this book would neither be necessary nor possible'. The only 2 people I grew up idolizing are still with us, Daniel Lednicer and David Nichols. Both have encouraged me, discussed serious research, lab-culture and tittle tattle with me and both have placed my safety as a matter they are concerned about. Please don't bombard them with vacuous communications but if you discover a novel compound within their realms of expertize then they really are interested. Even Derek P. Reynolds (he who designed isotilidine) was interested to know that a 2-step synthesis was possible based on a 2016 paper. I'm nobody special but I am polite and I am courteous and as I get older, youngsters do contact me for information and while I am flattered, it is their education and helping them become better than me is my goal. In short - I always want to be the most stupid person in the room; that way I have the most to learn from others.
Limpet_Chicken
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Can't say as novel steroids are an interest of mine. Neurosteroid GABAergics, yeah, those would, but I've never been into anabolics, or corticosteroids, although I did do some research looking into ACTH secretagogues or ACTH receptor direct agonists, although not for myself, rather, that was for my stalker, who has problems due to a very low ability to produce ACTH, and I wanted to help her. I did find a suitable melanocortin receptor agonist, but she decided against it, spent a fair few years researching that one, but its as close to steroid biochem as I've ever gotten to. (not that I was in any offended or saw it as her wasting my time, because I love her dearly, she's one of very few people I'd either spend the rest of my life with given the opportunity, or give my life for her. A very, very special lady. 53, gorgeous long dark hair, classically autistic, super-sexy and delightfully spesh, bright, sparky and fiery as hell. A very determined, dedicated kind of lady, the kind of person who when she sets her heart on something, she sees it through to the end, and won't be swayed 
)
How do relative stabilities of beta-keto phenethylamines and BK-amphetamines compare for compounds differing only into the chain length?
Wasn't indopan also AET rather than AMT? and AET, IIRC has some..issues. Specifically, although rare, potentially deadly agranulocytosis.
Haven't looked into BK-DON, although if I do, chances are it'll have to be protected as the pthalimidopropiophenone
)How do relative stabilities of beta-keto phenethylamines and BK-amphetamines compare for compounds differing only into the chain length?
Wasn't indopan also AET rather than AMT? and AET, IIRC has some..issues. Specifically, although rare, potentially deadly agranulocytosis.
Haven't looked into BK-DON, although if I do, chances are it'll have to be protected as the pthalimidopropiophenone
The ketone moiety changes the activity more that people realize. The N,N-dimethyl is just as potent a stimulant because of O: N: interaction. I remember in about 1994 that the 3-carbon analogue of MDPV turned up on the German market. As people know, an N-pentyl or phenylethyl provide the most active members of the class... that second aromatic shows it's a lipophilic pocket and (roughly) the active conformation. That is why isophenidine is just about the right balance of DRI & NMDA activity. I remain uncertain that ring-substitution of the alpha aryl is a good idea. You cannot just take the ACA QSAR and apply it. I know because I tasted the o-Cl, m-MeO, m-OH, p-MeO and so on.
Limpet_Chicken
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Interesting about the lone pair interaction between O:/N:, I had been wondering why the likes of N,N-diethylcathinone was such a popular drug at one point given the drastic loss in potency of for example, N,N-dimethylamphetamine with respect to the secondary amine counterpart, and also chain length increases causing a decrease in weight potency, although with a subjective improvement IMO in the case of N-monoethylamphetamine, despite its lower overall potency compared to meth, it is smoother, a more pleasant ride, and still a fair bit more effective than straight amphetamine.
Clubcard, here's a question for you. With certain pentylated amphetamine analogs, there is some rather unusual activity, specifically aryl-2-pentanes having a 2-propylamino group. These act as phasic neurotransmitter release-promoting agents, specifically targeting phasic release over inducing tonic release and dumping of neurotransmitter. Is it known if there are any cathinones having similar effects (or other ligands at all, with this unusual neurotransmitter releasing profile)? although obviously it would be quite impossible to make an analog of BPAP or PPAP with the double-bonded oxygen of a cathinone at the beta-carbon, given C is tetravalent. Isn't an ester group a potential bioisostere of a keto C=O ?
What do you mean by 'ACA'?
Clubcard, here's a question for you. With certain pentylated amphetamine analogs, there is some rather unusual activity, specifically aryl-2-pentanes having a 2-propylamino group. These act as phasic neurotransmitter release-promoting agents, specifically targeting phasic release over inducing tonic release and dumping of neurotransmitter. Is it known if there are any cathinones having similar effects (or other ligands at all, with this unusual neurotransmitter releasing profile)? although obviously it would be quite impossible to make an analog of BPAP or PPAP with the double-bonded oxygen of a cathinone at the beta-carbon, given C is tetravalent. Isn't an ester group a potential bioisostere of a keto C=O ?
What do you mean by 'ACA'?
Sorry - Aryl cyclohexyl amines. I know the class you mean but Reaxys only comes up with pyrovalerone analogues. Swapping the N-pentyl for a 1-amino-1,2-diphenylethane moiety will almost certainly work (and better LogP) but I always throw on a metabolically labile moiety so I can ensure of metabolism has no hidden nasties. P-Me worked well, indane no better, avioded using benzofuran (epoxide = bad) but didn't get to methylenedioxy. Keep it as close to an agent that has seen commercial use, take fluid samples and put them through NMR & GC-MS so you KNOW what is going on. It is a shame - almost nobody REALLY ensures intrinsic safety..... just us two, I think.
Limpet_Chicken
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NMR/GC isn't an option for me, I'm not rich like some folk. Not to say I'm not safety conscious, or that I'm living in the stone age, but all the same, sadly I don't have a money tree in the back garden. Thats what you get for being (not that I had much choice in the matter) an autodidact. Although on the flip side, at least my chosen path, is always guaranteed to be mine own.