Recruiting Seeking people with experience with both 5-MAPB and MDMA for a web survey

[MBaggott]

Hi, I'm Matthew Baggott, a neuroscientist who studies MDMA-like drugs and how they can be made safer, more effective, and more accessible. I'm also CEO of Tactogen, a public benefit corporation developing novel MDMA-like medicines.

I've put together an anonymous questionnaire to gather information on 5-MAPB and how it compares to MDMA. If you've used both drugs alone (i.e., without taking other substances at the same time), I'd love for you to fill out this questionnaire (link) .

The questionnaire is under 75 questions long and may take 25 minutes to complete.

The basic goal is to collect information on the human effects of 5-MAPB, which is poorly studied. I'm particularly interested in documenting whether 5-MAPB shares the therapeutic potential of MDMA.

The survey will be open for about 3 months or until it receives 200 responses, whichever comes first.

This project was examined and declared exempt from the need for approval by the Western IRB.

If you have any questions or comments, I can be reached here or via the email on the first screen of the questionnaire. Thanks!

Click here for questionnaire.

 

[AlsoTapered]

Ah - Tactogen holds the patent on 5-MAPB.

We found that 3,4-methylenedioxy aminorex (MDAR) to be much more active as was (R) 7,a-dimethyltryptamine.

 

[MBaggott]

Ah - Tactogen holds the patent on 5-MAPB.

We found that 3,4-methylenedioxy aminorex (MDAR) to be much more active as was (R) 7,a-dimethyltryptamine.

5-MAPB is unpatentable. Tactogen has pending patents on nonracemic mixtures of many benzofurans, including 5-MAPB. Unlike MDMA, where the R is close to inactive, both enantiomers of 5-MAPB (and many benzofurans) are potent with differing activity, such that nonracemic mixtures produce novel experiences. Tactogen is mainly interested in novel benzofurans (and other structures) rather than 5-MAPB because 5-MAPB produces long term 5-HT depletions similar to those from MDMA. I suspect both MDMA and 5-MAPB are similar in their long term serotonergic effects. 5-MAPB is still important to study, in part because people are using it.

Do you think MDAR and R-7-methyl-alphaethyltryptamine are more therapeutic?

 

[AlsoTapered]

5-MAPB is unpatentable. Tactogen has pending patents on nonracemic mixtures of many benzofurans, including 5-MAPB. Unlike MDMA, where the R is close to inactive, both enantiomers of 5-MAPB (and many benzofurans) are potent with differing activity, such that nonracemic mixtures produce novel experiences. Tactogen is mainly interested in novel benzofurans (and other structures) rather than 5-MAPB because 5-MAPB produces long term 5-HT depletions similar to those from MDMA. I suspect both MDMA and 5-MAPB are similar in their long term serotonergic effects. 5-MAPB is still important to study, in part because people are using it.

Do you think MDAR and R-7-methyl-alphaethyltryptamine are more therapeutic?

WO2021252538A2 - Advantageous benzofuran compositions for mental disorders or enhancement - Google Patents

Pharmaceutically active benzofuran compositions for the treatment of mental disorders or for mental enhancement, including for entactogenic therapy. The present invention also includes benzofuran compounds, compositions, and methods for generally modulating central nervous system activity and...

patents.google.com

Better tell PubChem they got it wrong.

But the 5HT2 isomer of 7,a-DMT while patented, isn't patented as an entactogen. Nor is 3,4-MDAR as far as I know. As a putative anoretic, yes, but not as an entactogen.

 

[MBaggott]

WO2021252538A2 - Advantageous benzofuran compositions for mental disorders or enhancement - Google Patents

Pharmaceutically active benzofuran compositions for the treatment of mental disorders or for mental enhancement, including for entactogenic therapy. The present invention also includes benzofuran compounds, compositions, and methods for generally modulating central nervous system activity and...

patents.google.com

Better tell PubChem they got it wrong.

Anyone can read that the claims all say "An enantiomerically enriched mixture of..." Like I said, the IP here is mainly on novel nonracemic mixtures. Existing molecules can't be patented. 5-MAPB will always be public domain.

Tactogen is a public benefit corporation that has the goal of making transformative medicines safer, more effective, and more accessible. We are seeking novel solutions that address the limitations of MDMA; this necessarily builds on existing knowledge.

 

[AlsoTapered]

Anyone can read that the claims all say "An enantiomerically enriched mixture of..." Like I said, the IP here is mainly on novel nonracemic mixtures. Existing molecules can't be patented. 5-MAPB will always be public domain.

Tactogen is a public benefit corporation that has the goal of making transformative medicines safer, more effective, and more accessible. We are seeking novel solutions that address the limitations of MDMA; this necessarily builds on existing knowledge.

I in no way denegrated Tactogen or suggested that it's aims were not noble. I merely pointed out that PubChem DOES list racemic 5-MAPB as being patented. I also noted other classes that do not appear to be thus patented and which Tactogen might benefit from.

Dave Nichols has the QSAR of the ring-substituted aminorex derivatives but even then, it only details the racemate. As for 7,a-DMT, it was amazingly MISSED in the Upjohn patents of the 1960s.

Since I have had the chance to try all of the above, it's my opinion that while MDAR is by far the most potent entactogen, 7,a-DMT has a nice, linear dose/response curve. Maybe the benzofuran homologue of that is of interest?

 

[AlsoTapered]

I am indeed impressed. I presume that since you are keen to elicit optically pure materials, you also discovered that the MDAR homologues are useful.

Example 13 of the original Poos patent deals with the MD derivative, but as you see - he only considers them as anoretics (and racemates).

I'm also very impressed that you didn't go for the synthetically simpler 4-MAR derivatives. Dave Nichols warned us that they have significant MAOI activity and so we avoided them... not that we enjoyed working with BrCN much.

It would be interesting to know if your derivative reduces or eliminated 5HT2b affinity of aminorex as this can result in heart-valve damage.

It's nice to share!

 

[G_Chem]

I very curious to know more about the different optical enatiomers of 5-MAPB. It sounds like there’s been some research already, is this something that can be shared here?

-GC

 

[MountainTrails]

Interesting stuff. I'm following along, and I guess mostly interested in how the various compounds address the anxiogenic nature of many comeups. For me, for example, on MDMA they can be horrific. For real. An empathogenic medicine that minimized that would be nice.

 

[MBaggott]

I very curious to know more about the different optical enatiomers of 5-MAPB. It sounds like there’s been some research already, is this something that can be shared here?

-GC

We've presented a little at conferences and are working on publishing papers. At a high level: Both enantiomers are active entactogens. EC50s for release of DA, NE, and 5-HT are all below 250 nM. The R is more serotonin biased than the S. Based on the pharmacological profile, I think S-enriched mixtures might be preferred for some uses to MDMA itself and might be reminiscent of a 'cleaner' version of what you've seen with MDMA+5-MAPB.

 

[AlsoTapered]

I believe a few examples of MDMA tablets what were shown to contain 65% (S) and 35% (R). Only showed up in 1 batch found in H
Germany (if memory serves).

 

[Phobos]

I believe a few examples of MDMA tablets what were shown to contain 65% (S) and 35% (R). Only showed up in 1 batch found in H
Germany (if memory serves).

Do you know if it had to be done intentionally by adding more steps to the synth or if it could be a normal synth done with a particular precursor?

 

[AlsoTapered]

Do you know if it had to be done intentionally by adding more steps to the synth or if it could be a normal synth done with a particular precursor?

Nobody knows. I GUESS that someone tried to produce a batch that was significantly stronger/better although IF someone has find a direct route from the gliycidate ester (which MAY be chiral) then you would end up with the chiral product. I did look and could not find such a route, but that just shows MY limitations.