Pharmacology Benzos - Further

[AlsoTapered]

I asked myself it it's possible to make something significantly more potent than flunitrazolam. It is, in fact given the affinity data it would appear that it's possible to make a chiral derivative that is an order of magnitude more potent.

I'm not about to state what it is, but I'm sure my BL friends will know. The nitro homologue of brotizolam is OBVIOUS but looking at the patents it's only about x2 brotizolam and boy is it complex to make.

So without naming, can you think of any benzodiazepine that is active at 100ug? I add that their are several and all chiral, but the improved affinity and LogP really do suggest that it's not only possible but possible to avoid the toxicity of the classic nitrobenzodiazepines and to avoid significant a1 affinity (the receptor that means when mixed with opioids, it KILLS).

I am not bragging or indeed offering to sell the design. I'm just interested to know how many others have looked closely at affinity, looked into the work of Dr (captain) James Cook and realized that indeed, these things CAN be more potent than LSD.

It's purely an intellectual exercise. Consider LogP, affinity and metabolism.

So if you say 'yes', I guess you have the same solutions as I. It's not a show and tell. You have your research, I have mine. I do NOT want these designs to reach the organized criminals who seek to make money at the expense of end users. I have warned of flunitrazolam... at great length. So this is just me seeing the doom. I just hope others are feeling the same...

The power to harm others isn't a good thing. It weighs on me. But if I'm not alone, at least I know I'm not the only one.

 

[SpiralusSancti]

Am I wrong or would nitrobenzodiazepine designed to be active at microgram range result in a compound that would have no significant hepatoxicity at normal doses (sub mg range)?

Being in control of production, distribution and dosage of something and ensuring all HR protocols are used might be better than postponing occurrence of something by unknown but not likely very long time. Especially with current drug policies it is possible to willingly get something banned before it creeps into black market and makes a lot more damage than as an RC in appropriate form for something that potent. We have seen how for multiple substances literally only one significant source is available if low price and big enough production capacity is realised. I highly doubt that we’ll ever see situation where most of “street benzo” is in fact RC and not just regular benzo production diverted for black market. I’m confident that no matter how good etizolam is, it would have never become a such success if it wasn’t Rx medicine in big markets already.

 

[AlsoTapered]

Hi - now that is an interesting question. I would have presumed that since flunitrazepam is x10 the potency of nitrazepam, it would be x10 less toxic BUT in that case, they were almost equally as toxic. That nitro group can be metabolised to something toxic - maybe it's toxic AT the GABA receptor and so while you need less of a material with high affinity, the metabolite's higher affinity cancels it out.

As you know, I looked at a very large Swedish study and in cases of intentional overdose, the units prescribed in a given region were more of a guide than WHICH benzo was prescribed.

It's possible to increase activity by a further order of magnitude by certain modifications. It's a BIT more costly to make (say 10%) but it's the compound I would be looking for right now to spot the organised criminals who now control RC benzos.

Imagine a compound that's active at 0.01mg. I wouldn't say it unless I had the documents and affinity data sat right in front of me. I'm also stuck because I cannot tell people to watch out for it because then the RC vendors would also know.

 

[AlsoTapered]

BTW as for 'further', their are some super-agonist derivatives. I don't know if overall potency differs, but we made a super-agonist variant of pyrazolam and it was about twice as potent, had a faster onset and longer duration. We dumped it because we noted that people would take it 'for fun' rather than just to treat anxiety... so we saw 'high abuse potential and that in a class we had worked so hard NOT to be abusable.

The LogP and affinity were significantly higher so we considered 0.25mg mg dose-units. But the subjects given 100 pyrazolam used them in around 160 days. With the derivative, they were gone in a mean of 65. Now THAT is a warning!

 

[SpiralusSancti]

We dumped it because we noted that people would take it 'for fun' rather than just to treat anxiety...

Imo and ime benzos are, no question, a group of drugs that leads to most problems if they are recreational; be it for certain person or cuz of specific compound. Etizolam quickly lead to profund life changes, that seemed just great and welcomed while it doesn't become bloody obvious I fucked up. Only other drug that caused that to me (not realizing I’ve overdo it until it’s too late) is coke. And to make things more, sad, I guess, I always thought benzos or coke could never fuck me up as I’m not a huge fan. And only third one I believe could do that too, is tobacco.

 

[AlsoTapered]

Wait until the DEA starts getting to vendors. It will be darkweb only and you get what you are given.

I know multiple people who are spending $150 on opioid habits... so these RC vendors realize that their is MORE profit in users having a $150/day benzo habit.

I keep trying to warn people but dependant users don't WANT to know. So I foresee a lot of deaths and ER visits... and given the sheer LEVEL of dependence involved, it's not like a doctor is going to write for 36 x 10mg per day...

In short, it didn't make the news like fentanyl but it's sure going to be worse.