What does the numbness in NBOMe blotters come from?

[onetwo]

Well in many RCs and specifically NBOMes, the blotters have that strong taste that's kind of numbing and tastes like novocaine. Just wondering if you guys knew where it came from, whether the actually chemical itself? Or in the way it's complexed or something? Because I seem to of been using the measure of if the blotter still tastes like novocaine/bitter of when I can spit it out and just wondering if that makes any sense?

 

[freedstar]

It's the chemical. Holding it in until you stop tasting it would be the best.

 

[Sepher]

It's not the complexing. HPBCD is sweet tasting ( it's a kind of sugar, right? ), the bitter taste is the NBOMe. I actually think it has a slightly metallic taste, 25I anyways, more than bitter. If you're still tasting it I'd suggest you still have actives on the blotter to absorb though I doubt you're gonna wring every last bit out. How long you leaving them in? I get very little taste left after 45-60 minutes which is probably way more than I need to keep them in but no hardship, may as well leave them there but there is always a little bit of a taste left.

 

[IamMe90]

There is absolutely no need to leave in the blotters longer than 15, 20 minutes max if you are holding them in the proper area and retaining some saliva. I've started tripping balls within 25 minutes of putting the blotters in my mouth.

 

[Ligaturd]

I would say that there is a need, if you can still taste the 25x compound coming from the blotter then that suggests that the blotter still has actives in it and maybe you should lower your dose if the full dose in the blotter wasn't needed to get you where you wanted to be.

 

[freedstar]

There is absolutely no need to leave in the blotters longer than 15, 20 minutes max if you are holding them in the proper area and retaining some saliva. I've started tripping balls within 25 minutes of putting the blotters in my mouth.

There is a need if you want the entire dose. I've tasted tabs that last way past 30 minutes. It's true you start tripping pretty fast, maybe 15 or 20 minutes, so it's up to you to decide how long you feel like holding them in.

 

[Solipsis]

One theory:

I have compared the chemical structure of local anaesthetics like lidocaine, while they are amides instead of secondary amines there is some resemblance to the actual NBOMe part of those drugs (i.e. the substituted N-Benzyl part), the part that is similar in those anaesthetics is also the part the different ones in that class have in common. Additionally, it is also the part in NBOMe-type drugs that is special to them, the part the corresponding 2C-X does not have.

So I'd say it's at the very least plausible that this terminus of the molecule is what is essential for the anaesthetic action: it may fit in calcium channels in nerve cell membranes and block them so that no signal runs along that nerve. The kind of signal regulating general sensation of pressure, temperature and particularly pain... the result being local numbness.

Logical deduction IMO points towards this.

I do however find it suspicious that this numbness occurs at such low doses.

 

[Jesusgreen]

There is absolutely no need to leave in the blotters longer than 15, 20 minutes max if you are holding them in the proper area and retaining some saliva. I've started tripping balls within 25 minutes of putting the blotters in my mouth.

In my experience, leaving them in longer has a dramatic effect. Leaving a 1mg blotter in for 20-30 minutes produced a decent ++ with some nice visuals, while leaving one of the same blotters for just over an hour led to a very strong +++ almost close to a ++++ with the visuals so intense I saw my friend turn into a giant tarantula in front of me.

I've noticed others reporting that holding the blotters in longer is beneficial. Given that it's not orally active, you can fairly safely assume that if you can still taste any chemical on the blotter when you swallow it - there's substance going to waste.

---

As for the numbness, possibly localised vasoconstriction? Any of us with experience with NBOMes know how generally vasoconstricting the substances can be, so it wouldn't be all that surprising to me if they did this locally causing numbness in the areas they touch too.

 

[SerotonergicHaze]

Could be Na+ channel blockade?

Many local anesthetics produce seizures, convulsions, cardiac arrest etc in overdose. Perhaps this may explain why 25I-NBOMe is more toxic than other psychedelics such as LSD and Psilocin (although I think full agonism @ 2A as opposed to partial with the latter two plays a big role)

It's structure appears to bare some vague resemblance to amino amides.

I had a quick gander on pubmed, and sadly since this compound is so new, I don't think anyone has bothered to assay it at the Na channel

 

[IamMe90]

In my experience, leaving them in longer has a dramatic effect. Leaving a 1mg blotter in for 20-30 minutes produced a decent ++ with some nice visuals, while leaving one of the same blotters for just over an hour led to a very strong +++ almost close to a ++++ with the visuals so intense I saw my friend turn into a giant tarantula in front of me.

I've noticed others reporting that holding the blotters in longer is beneficial. Given that it's not orally active, you can fairly safely assume that if you can still taste any chemical on the blotter when you swallow it - there's substance going to waste.

---

As for the numbness, possibly localised vasoconstriction? Any of us with experience with NBOMes know how generally vasoconstricting the substances can be, so it wouldn't be all that surprising to me if they did this locally causing numbness in the areas they touch too.

Well, I dunno then, I've consistently tripped absolute balls on normal doses of the drug while only holding the blotters for 15-20 minutes. I'm talking high end, +++ terribly intense experiences. Maybe I've done particularly well retaining the saliva or keeping the blotter in place? Oh well, glad that I don't ever have to hold them in longer than 20 minutes haha, it's a disgusting and annoying process.

 

[tryp2fun]

Could be Na+ channel blockade?

Many local anesthetics produce seizures, convulsions, cardiac arrest etc in overdose. Perhaps this may explain why 25I-NBOMe is more toxic than other psychedelics such as LSD and Psilocin (although I think full agonism @ 2A as opposed to partial with the latter two plays a big role)

It's structure appears to bare some vague resemblance to amino amides.

I had a quick gander on pubmed, and sadly since this compound is so new, I don't think anyone has bothered to assay it at the Na channel

I agree. The numbness feels like a local anesthetic, not just the result of local vasoconstriction.

 

[nooneman]

Could be Na+ channel blockade?

Many local anesthetics produce seizures, convulsions, cardiac arrest etc in overdose. Perhaps this may explain why 25I-NBOMe is more toxic than other psychedelics such as LSD and Psilocin (although I think full agonism @ 2A as opposed to partial with the latter two plays a big role)

This is exactly what I was thinking. Maybe differences in overdose depend on differences in response to local anesthetics. Differences in local anesthetic response are not rare.

However, Novocain works great for me, but 25i doesn't cause numbness for me, or at least none that I've noticed. Maybe there was a little, but I really didn't notice.

 

[PhyllipThylamine]

So perhaps the NBOME series have some annalgesic effects? This might be handy in future, if psychedelic therapy continues to gain (REgain) ground. If tripping is sometimes helpful for people with terminal illness, the added effect of analgesia may be convenient. I mean, if there's some pain reducing effects, as well as being an hallucinogen, it's possible folk with painful, terminal illness being given psychedelic therapy might be given less common analgesic while undergoing psychedelic therapy. This could increase the beneficial psychedelic effects without dampening them down with a morphiod or whatever for pain managment.

 

[Solipsis]

So perhaps the NBOME series have some annalgesic effects? This might be handy in future, if psychedelic therapy continues to gain (REgain) ground. If tripping is sometimes helpful for people with terminal illness, the added effect of analgesia may be convenient. I mean, if there's some pain reducing effects, as well as being an hallucinogen, it's possible folk with painful, terminal illness being given psychedelic therapy might be given less common analgesic while undergoing psychedelic therapy. This could increase the beneficial psychedelic effects without dampening them down with a morphiod or whatever for pain managment.

I think you are misunderstanding (or are ignorant to) the important differences between local anaethesia and central analgesia. The former only happens at the spot the compound is applied and it does not only stop the sensation of pain but also general feeling i.e. numbness. I don't think calcium/sodium channel blockade by NBOMe's could possibly have use for something like palliative care. It is restricted to topical places where there is high enough concentration i.e. where the blotter sits on the gums, you cannot put it on a wound. And the psychedelic effects probably produces hypersensitivity that overrides any local numbing.

For the terminally ill, assuming they have a painful condition here, what is needed is a centrally acting drug. I'm not sure how clearheaded one can remain while heavily treated with analgesics... generally speaking these are depressants. Any 'terminal' trip is probably still best produced by a separate substance, apart from practicality I don't see why we would specifically need a drug that can take of the psychedelia and pain management - considering different levels of psychedelia and needed pain killing this is impractical even if there were a pharmacological basis for the idea.

Sorry.

 

[Jesusgreen]

Well, I dunno then, I've consistently tripped absolute balls on normal doses of the drug while only holding the blotters for 15-20 minutes. I'm talking high end, +++ terribly intense experiences. Maybe I've done particularly well retaining the saliva or keeping the blotter in place? Oh well, glad that I don't ever have to hold them in longer than 20 minutes haha, it's a disgusting and annoying process.

Don't get me wrong, you'll get a solid trip from holding them for 20 minutes, but try taking say 3/4 (or less) of your usual dose and holding the blotter there for 40+ minutes and see the difference. You'll most likely trip just as hard as you were from your previous dose.

If the blotter still tastes bitter there's almost certainly some of the drug going to waste if you swallow it already.

Regarding the numbness, I noticed 25C produces significantly more numbness in my mouth at a similar dose to 25I, it also produced significantly more general vasoconstriction throughout the trip.

 

[jhoppa]

apart from practicality I don't see why we would specifically need a drug that can take of the psychedelia and pain management - considering different levels of psychedelia and needed pain killing this is impractical even if there were a pharmacological basis for the idea.

LSD was actually tested for analgesic properties and found to work better than Demerol or Dilaudid, in addition to its psychotherapeutic benefits. About a third of the way down, the relevant study is cited.

 

[atara]

I'd say neuronal sodium channels are a definite antitarget in terms of making a safe and effective psychedelic drug. It is generally hypothesized that cocaine's toxicity is primarily a result of its local anaesthetic effects rather than its psychoactive ones. This was the motivation for the development of the phenyltropanes, which are not local anaesthetics and are expected to be safer than cocaine. Local anaesthetics put a significant amount of stress on the heart: if this is true, it could explain how the deaths on 25I occurred.

 

[any major dude]

Interesting atara, I've been curious as to the physiologic COD in those instances, as it didn't appear to be bromo-Dfly like vasoconstriction. My speculation was probably something ischemic or possibly a heart attack.

 

[Solipsis]

LSD was actually tested for analgesic properties and found to work better than Demerol or Dilaudid, in addition to its psychotherapeutic benefits. About a third of the way down, the relevant study is cited.

Excellent point. Hadn't thought of it like that, I guess not everything is transparant through pharmacology.

Unfortunately it seems local anaesthesia is not without risk as atara points out... now that he mentions it I do recall lidocaine being quite unhealthy / dangerous taken enterally.

 

[atara]

Local anaesthetics are toxic indeed.

However, the consensus among People Who Know Things, now that I've had the chance to ask them, is that the likelihood of 25x having significant affinity for the local anaesthetic binding site is effectively nil -- the structure-activity relationship for Na+ blockers requires an ester or amide linkage of some sort -- doubly so because at ordinary doses they'd have to be extraordinarily potent to produce any noticeable activity. So local anaesthetic activity as an explanation of 25x toxicity seems to be right out -- and we'll have to keep looking.