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Pharmacology How drugs affect the workings of the human body.

 
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  #1  
Old 30-01-2010, 20:16
Crazy Insane Sanity Gold member Crazy Insane Sanity is offline
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Low dose psychedelic tolerance?

OK, so common sense would tell me that if one were to take a small dose of a psychedelic (say half a hit of blotter) it'd take less time for the tolerance to dissipate. I was curious if this is actually true, or if anyone had any more specific details on what would happen though.

If Swim were to take just enough of a traditional 5-ht2a agonizing psychedelic to just reach threshold levels, would he be able to do the same thing the following day? How long could this process be continued, and at what intervals between what level of doses?

I'm not asking this because Swim wants to try. I'm asking because Swim and I would like to know without actually trying.
  #2  
Old 30-01-2010, 23:32
Jasim Gold member Jasim is offline
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Re: Low dose psychedelic tolerance?

I wonder if one could take a lower dose, and use other supplements to increase the effectiveness, if the tolerance would be less and dissipate more quickly. Interesting question posed Crazy.
  #3  
Old 31-01-2010, 00:14
Crazy Insane Sanity Gold member Crazy Insane Sanity is offline
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Re: Low dose psychedelic tolerance?

Thanks Jasim! Actually I had the same thought and started a thread on it while ago...I believe, if I remember correctly, you were the only person who responded to it.

Crazy Insane Sanity added 35 Minutes and 55 Seconds later...

Sorry, I misread your post. Still an interesting thought though! I suppose it would depend on how it's increasing the drugs effectiveness. Like if it's preventing the metabolism of the substance, then it would likely still downregulate the receptors...but perhaps there is another mode of action that could work?

Last edited by Crazy Insane Sanity; 31-01-2010 at 00:25. Reason: Automerged Doublepost
  #4  
Old 07-02-2010, 07:52
gergmacmillan gergmacmillan is offline
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Re: Low dose psychedelic tolerance?

from a pharmacological point of view, swim would think that swiy's initial idea is most likely correct, as it seems to swim that the building up of a tolerance most likely has to do with extended plasma levels of a substance in the body/brain. swim is pretty sure that research has shown that tolerance to lsd (among other drugs that effect the 5HT receptors) is most likely caused by a decrease the number of 5HT receptor sites in the brain (though whether or not these sites regenerate is still unclear {see the work of Dr. David Nichols}). with less receptors available for lsd molecules to bind to, there is less of a perceived effect (aka a tolerance). swim was unable to find any studies on the particular question posed by swiy, however he would think that it is a logical conclusion to draw that if there is more lsd in your system, then there is a longer exposure to this effect, (as consuming higher doses will mean there is more active chemical in your system for longer) and with smaller doses, the potential for development of a tolerance will be higher. from personal experience swim is unsure (as he has generally consumed relatively high doses, around 100 mics at a minimum and up to a milligram maximum if he had to guess). as a side note, another thing he has noticed is that the visual/auditory and overall PERCEPTUAL changes brought on by an lsd can almost always be brought about by higher and higher doses, however the profoundness of a trip is always depleted with tolerance (basically you can always get stoned in an lsd way, however with regular usage, you will almost always get less and less of a profound, and possibly life changing trip)

hope this helps answer your question
  #5  
Old 07-02-2010, 11:20
69Ron 69Ron is offline
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Re: Low dose psychedelic tolerance?

It will vary by the compound in question. Some phenethylamine psychedelics actually exhibit reverse tolerance.

Last edited by 69Ron; 07-02-2010 at 20:37.
  #6  
Old 07-02-2010, 14:35
Crazy Insane Sanity Gold member Crazy Insane Sanity is offline
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Re: Low dose psychedelic tolerance?

Quote:
Originally Posted by 69Ron View Post
It will vary the compound in question. Some phenethylamine psychedelics actually exhibit reverse tolerance.
Could you elaborate on this statement?
  #7  
Old 07-02-2010, 20:45
69Ron 69Ron is offline
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Re: Low dose psychedelic tolerance?

Quote:
Originally Posted by Crazy Insane Sanity View Post
Could you elaborate on this statement?


Some psychedelics like mescaline do not show much tolerance, others show “reverse tolerance”. A small dose of mescaline taken everyday in some people, not all, will cause INCREASED effects after several days so that taking a smaller dose is actually more effective. This is caused by buildup of the drug and a lack of tolerance to it. But with drugs like LSD, the opposite happens. Tolerance to LSD builds rapidly and lasts several days. If you take 50 micrograms of LSD everyday for a week, it will eventually have no effect at all. If you take 100 mg of mescaline everyday for a week, at the end of the week some people will have very strong effects from it. This is called “reverse tolerance”. It’s actually just a buildup of drugs in your system with your body not developing tolerance to the drug.

So it depends on the compound in question. In general phenethylamine psychedelics like mescaline show either very little tolerance build up or reverse tolerance, while tryptamines like LSD (LSD is actually both a tryptamine and phenethylamine) show rapid tolerance build up.

Also another factor is the duration of the drug. For example, DMT shows rapid tolerance build up, but also tolerance to it is lost rapidly, so that it can be used everyday with no tolerance build up, but if used every 5 minutes 100% tolerance to it will happen after a short while. But tolerance to it only lasts about 30-60 minutes (or longer in some people).

So this is a complex question.
  #8  
Old 08-02-2010, 15:13
Jasim Gold member Jasim is offline
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Re: Low dose psychedelic tolerance?

Don't mean to nitpick, but LSD is not considered a phenethylamine. Take a look at the structure, the phenethylamine is just not there, unless you're referring to the indole, but that's with ALL tryptamines.




But that's interesting about phenethylamines not causing tolerance, I've r heard that before.
  #9  
Old 09-02-2010, 02:40
69Ron 69Ron is offline
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Re: Low dose psychedelic tolerance?

Jasim, you are absolutely wrong. I know what I'm talking about. It is there. Look again.

Here is phenethylamine:


This shows LSD's phenethylamine structure in red:


Here's tryptamine:


This shows LSD's tryptamine structure in green:


It's as plain a day. It's both. I'm sure you see it in the structure now.

This is why LSD has effects that are similar to both mescaline and psilocybin. Mescaline and psilocybin are more like LSD than like each other because of the structural relationship they both have in common with LSD. Mescaline and psilocybin only share a benzene ring. They don't share anything else. LSD has effects that are unique to phenethylamines which psilocybin doesn't have, and LSD has effects that are unique to tryptamines which mescaline doesn't have. It's sort of a cross between the two classes of psychedelics.

Because LSD is both a phenethylamine and a tryptamine, its best to call it an ergoline to be more clear about what class it belongs to. An ergoline is both a phenethylamine and a tryptamine. While it's very popular to misrepresent it as a tryptamine, its an ergoline, and made from ergolines like lysergic acid and never made from tryptamine or phenethylamine.

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Very informative.

Last edited by 69Ron; 09-02-2010 at 09:42.
  #10  
Old 09-02-2010, 14:19
Jasim Gold member Jasim is offline
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Re: Low dose psychedelic tolerance?

Wow, how did I miss that before?! Thanks for pointing that out!
  #11  
Old 10-02-2010, 03:11
69Ron 69Ron is offline
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Re: Low dose psychedelic tolerance?

Jasim, don’t feel bad for not seeing it there. Most people don't see it until it’s made obvious by that picture. For a long time I didn’t notice it either, until I was playing around with some molecular models and suddenly noticed it there and was amazed to see it. It’s funny how most people don’t talk about LSD also being a phenethylamine and just classify it as a tryptamine. Even people like Alexander Shulgin call LSD a tryptamine. I don't know who got it started to call LSD a tryptamine, but it's really not correct. Calling LSD a tryptamine implies that it's also not a phenethylamine. Tryptamines like DMT and psilocybin are serotonergic, and not dopaminergic, but phenethylamines are primarily dopaminergic. LSD is both serotonergic and dopaminergic, having the effects of tryptamines and phenethylamines.

About 50% of psychedelic users find LSD to be more like mescaline, while the other half finds LSD to be more like psilocybin. It’s funny how it affects people differently like that. For SWIM, LSD is more like mescaline than psilocybin. I guess SWIM is more sensitive to phenethylamines and so he feels those effects of LSD more than the tryptamine effects it has.

What I think is interesting is that mescaline and psilocybin show less tolerance than LSD does. If one takes the same dose of mescaline everyday for 1 week, the effects are either only slightly diminished or in some cases stronger. If one takes the same dose of psilocybin everyday for 1 week, the effects are very noticeably diminished but it’s still effective to a certain degree. But if one takes the same dose of LSD everyday for 1 week, it becomes completely ineffective.
  #12  
Old 11-04-2010, 10:32
gergmacmillan gergmacmillan is offline
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Re: Low dose psychedelic tolerance?

Quote:
Originally Posted by 69Ron View Post
Jasim, don’t feel bad for not seeing it there. Most people don't see it until it’s made obvious by that picture. For a long time I didn’t notice it either, until I was playing around with some molecular models and suddenly noticed it there and was amazed to see it. It’s funny how most people don’t talk about LSD also being a phenethylamine and just classify it as a tryptamine. Even people like Alexander Shulgin call LSD a tryptamine. I don't know who got it started to call LSD a tryptamine, but it's really not correct. Calling LSD a tryptamine implies that it's also not a phenethylamine. Tryptamines like DMT and psilocybin are serotonergic, and not dopaminergic, but phenethylamines are primarily dopaminergic. LSD is both serotonergic and dopaminergic, having the effects of tryptamines and phenethylamines.

About 50% of psychedelic users find LSD to be more like mescaline, while the other half finds LSD to be more like psilocybin. It’s funny how it affects people differently like that. For SWIM, LSD is more like mescaline than psilocybin. I guess SWIM is more sensitive to phenethylamines and so he feels those effects of LSD more than the tryptamine effects it has.

What I think is interesting is that mescaline and psilocybin show less tolerance than LSD does. If one takes the same dose of mescaline everyday for 1 week, the effects are either only slightly diminished or in some cases stronger. If one takes the same dose of psilocybin everyday for 1 week, the effects are very noticeably diminished but it’s still effective to a certain degree. But if one takes the same dose of LSD everyday for 1 week, it becomes completely ineffective.
swim would like to ask for clarification on the basis of some of swiy's statements (in the most respectful way possible, and out of curiosity alone, not in an attempt to say who is right or wrong)... first of all, swim would have to say that the structure-activity relationship mentioned for LSD doesn't seem to have pharmacological basis, and as far as he understands is an over-simplification. not only is the effect of LSD and psychedelics in general poorly understood (in terms of connecting structure/receptor relationships and the subjective experience), there are literally thousands of drugs that have the phenethylamine or tryptamine skeletons that are not psychedelic in any way at all, and many that produce no subjective effects in the user (the list of known non-psychoactive tryptamines/phenthylamines vastly outweighs the list of psychoactive compounds). further more, the binding of a drug to a receptor (either as an agonist, partial agonist, or antagonist) is rarely a comprehensive way to study the effects of a chemical outside of a physiological perspective (i.e. subjective alteration of consciousness) and does not at this time give any solid indication/qualitative analysis of psychoactivity. there is of course STRONG correlation between 5-HTa1 agonists and psychedelic effects, however at this time there exists almost no way of predicting the shades/degrees of effects based on receptor affinity/ physiological observations and there are many drugs that act similarly as agonists at this site which produce NO psychedelic or even psychoactive effects at all (which probably says alot about the general lack of understanding of the human mind/consciousness in general). a basic example of the lack of true understanding of these processes, is that 2-HT2a agonists (with specific/high affinity for that site) have been shown to at times produce psychedelic effects, and at times to produce no subjective effects at all (see gonzales-maeso study) and yes, swim knows that 2-HT is not the same as 5-ht, this merely illustrative comment. swim is not going to go further with this point, as the many hypotheses are far from proven, and is merely trying to show/remind people that these data aren't easy to correlate to effects, and that this is still a grossly understudied area (for its seeming relevance/application to the eventual qualitative understanding of consciousness).

not to put too fine a point on it again, but swim would like to note that while the molecular structures shown in one of swiy's previous posts SEEM to show that LSD is both a phenethylamine/tryptamine, this has no chemical/pharmacological basis. without posting images of his own, swim would like to point out that the skeleton of tryptamine is (according to the definition implied by swi69Ron's statement that LSD is 'based' on both tryp and phen) 'based' on the skeleton of phenethylamine (the only difference being tryptamine contains a pyrrole ring fused to the benzene ring)... according to what swim thinks he understands swi 69Ron to be saying, this makes all tryptamines also phenethylamines, which is simply not true. specifically referencing the molecular 'analysis' offered for LSD, the image-correlation is an example of pseudo-science (in swim's humble opinion), as it sure seems to make sense without any chem/pharm background, but is at best an oversimplification (the fact that the 'phen' part of LSD, and the 'tryp' part in swiys explanation are composed of the same atoms strikes me as a little odd/and doesnt make sense. does this mean swiy saying that any chemical with a benzene ring is a phenethylamine?). also, chemically speaking there is a huge difference between any molecular skeleton that is part of a greater structure and the original skeleton itself, and specifically in the case of LSD as a tryp/phen, the analysis given does not apply pharmacologically. the metabolic action/binding of a phenethylamine and tryptamine is most closely associated with the EXPOSED nitrogen group(the NH2, amine group)... in LSD, access to either of the two nitrogen atoms is blocked by two ethyl groups in one case, and a methyl group in the other case, meaning some metabolic action is needed to expose these nitrogens and giving no evidence of consistent action as a 'tryptamine' or 'phenethylamine' (which themselves have some/little subjective consistency, even among closely related analogs)

mescaline/ phenethylamines in general DO affect the dopaminergic systems (hence the stimulation commonly associated with these compounds and the related 3-carbon chained amphetamines), however many of the psychedelic amphetamines and phenethlyamines bind to 5HT receptors with high affinity, therefore the statement that they are primarily dopaminergic agonists (or dopaminergic in general) is also false/over simplified. there is no evidence to suggest that DRI (dopamine reuptake inhibitors) are responsible for psychedelic effects in any way, and the increased dopamine levels facilitated by these chemicals (of which amphetamine [where DRI effects form a positive feedback loop with dopamine releasing effects], cocaine, methylphenidate, and pcp are all examples) is most likely a cause of stimulation (dopamine is an excitatory neurotransmitter) and not much else. it should also be noted that serotonin receptors mediate a wide-range of neurotransmitters (including dopamine), as well as many hormones; this is a main piece of evidence linking 5HT receptors (specifically 1a) to playing a key role in psychedelic action (as there is simply SO MUCH going on with the activation of these receptors)

LSD is also a lysergamide (amide derivative of lysergic acid, which is itself derived from ergoline), not an ergoline itself, since this is an attempt to clarify the information presented.
swim feels he will continue to ramble away, and must cut himself short, but would like to make one last point: the 'observation' that LSD is 'more phen than tryp for some and more tryp than phen in others' (already stated as having little basis in fact), indirectly brings up a key point in relation to psychedelic experience with respect to the 'set' aspect of set and setting. if one has more experience with one class over the other, then it seems LSD would probably most closely resemble that class (in a general sense). in swim's experience, LSD is the psychedelic he has found he can control the most (as far as these things go =P), meaning he can shape a trip or trip with specific goals in terms of psychological exploration/resolution. this would seem to lend itself to the idea that LSD is subjectively experienced in a more 'malleable' way (and is philosophically beautiful since WE as a species synthesized this amazing chemical, as opposed to eating peyote or smoking DMT and having nature throw its chaotic visions our way... haha or something like that =D)
not trying to be inflammatory to swi 69Ron, but swim hates to see people mis-informed, and had to respond with even some very basic (but more accurate) simplifications of his own...
peace/hope this is not received in a negative way...

having gone back and read his posts, noticing swi69Ron has been somewhat forward in stating that several other swimmers are absolutely WRONG, and stating that he knows what he is talking about (which always makes swim suspicious b/c everybody should be humble with respect to their knowledge base, and quite frankly swi69ron doesn't seem to have much truly helpful information on this page). for example 100 mg of mescaline consumed with no tolerance will MAYBE push a threshold so swim not sure what going on with that comment about tolerance (unless you consume freebase, but swim has never come across free base mescaline), and despite most likely facing some negative feedback b/c swims rep< swi rons rep by a long way, he has to put this out there...
swi69ron: SWIY, sir, are absolutely wrong *based on the information presented here* and if you know what you are talking about *as you claim* swim would greatly appreciate a response with ANY sort of actual evidence of your claims. as a pharmacology student, swim does not claim to 'know what he is talking about' (when he does to some extent) and then proceed to act like it is true... when to put it bluntly, there is no evidence swiRon gave either chemically (TRUE chemistry) or pharmacologically coherent reasons for his claims. swim is trying to make it abundantly clear there is no 'holier than thou' aspect to his post, just REALLY got to him that swiRon is being taken as a solid reference (due to rep no doubt), when swim can see no evidence that this is true for this topic (again solely based on this thread)... all a matter of principle and please by all means respond as you see fit, swi69 Ron , but please dont ruin swims rep or something because this pissed you off... =/ peace

Last edited by gergmacmillan; 11-04-2010 at 10:54. Reason: re read 69Ron ;s post
  #13  
Old 12-04-2010, 02:49
Jasim Gold member Jasim is offline
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Re: Low dose psychedelic tolerance?

First of all, this is way off topic and really deserves a thread on its own, but I'm compelled to respond with my own thoughts. Wow, this is turning into a bad habit of mine to hijack CIS's posts, I do hope you don't mind.

Quote:
Originally Posted by gergmacmillan View Post
there are literally thousands of drugs that have the phenethylamine or tryptamine skeletons that are not psychedelic in any way at all, and many that produce no subjective effects in the user (the list of known non-psychoactive tryptamines/phenthylamines vastly outweighs the list of psychoactive compounds).
That is very true. A large part of it is very possibly due to the ability of such drugs to traverse the blood brain barrier. See my next comment.

Quote:
further more, the binding of a drug to a receptor (either as an agonist, partial agonist, or antagonist) is rarely a comprehensive way to study the effects of a chemical outside of a physiological perspective
That is very true, that is only one small aspect of the study of a drug. In reference to both this statement and the one above I would like to add that many known pharmacophores exist which are known to act on a given receptor. The idea that a phenethylamine pharmacophore acts on the dopaminergic pathway is very well established. Likewise for the tryptamine pharmacophore and serotonergic pathways. However, as you state below this is a gross oversimplification of what's really going on.

Quote:
(i.e. subjective alteration of consciousness) and does not at this time give any solid indication/qualitative analysis of psychoactivity. there is of course STRONG correlation between 5-HTa1 agonists and psychedelic effects, however at this time there exists almost no way of predicting the shades/degrees of effects based on receptor affinity/ physiological observations and there are many drugs that act similarly as agonists at this site which produce NO psychedelic or even psychoactive effects at all (which probably says alot about the general lack of understanding of the human mind/consciousness in general).

swim would like to note that while the molecular structures shown in one of swiy's previous posts SEEM to show that LSD is both a phenethylamine/tryptamine, this has no chemical/pharmacological basis. without posting images of his own, swim would like to point out that the skeleton of tryptamine is (according to the definition implied by swi69Ron's statement that LSD is 'based' on both tryp and phen) 'based' on the skeleton of phenethylamine (the only difference being tryptamine contains a pyrrole ring fused to the benzene ring)... according to what swim thinks he understands swi 69Ron to be saying, this makes all tryptamines also phenethylamines, which is simply not true.
A tryptamine by definition is an 'indole ethyl-amine'. That's like saying all indoles are therefore phenethylamines. Just confusing semantics, as is the comment below regarding lysergamides and ergolines.

Quote:
LSD is also a lysergamide (amide derivative of lysergic acid, which is itself derived from ergoline), not an ergoline itself, since this is an attempt to clarify the information presented.
More semantics. A lysergamide is just a more specifically defined ergoline.


Quote:
the analysis given does not apply pharmacologically. the metabolic action/binding of a phenethylamine and tryptamine is most closely associated with the EXPOSED nitrogen group(the NH2, amine group)... in LSD, access to either of the two nitrogen atoms is blocked by two ethyl groups in one case, and a methyl group in the other case, meaning some metabolic action is needed to expose these nitrogens and giving no evidence of consistent action as a 'tryptamine' or 'phenethylamine'
Quote:
mescaline/ phenethylamines in general DO affect the dopaminergic systems (hence the stimulation commonly associated with these compounds and the related 3-carbon chained amphetamines), however many of the psychedelic amphetamines and phenethlyamines bind to 5HT receptors with high affinity, therefore the statement that they are primarily dopaminergic agonists (or dopaminergic in general) is also false/over simplified. there is no evidence to suggest that DRI (dopamine reuptake inhibitors) are responsible for psychedelic effects in any way, and the increased dopamine levels facilitated by these chemicals (of which amphetamine [where DRI effects form a positive feedback loop with dopamine releasing effects], cocaine, methylphenidate, and pcp are all examples) is most likely a cause of stimulation (dopamine is an excitatory neurotransmitter) and not much else. it should also be noted that serotonin receptors mediate a wide-range of neurotransmitters (including dopamine), as well as many hormones; this is a main piece of evidence linking 5HT receptors (specifically 1a) to playing a key role in psychedelic action (as there is simply SO MUCH going on with the activation of these receptors)
Quote:
the 'observation' that LSD is 'more phen than tryp for some and more tryp than phen in others' (already stated as having little basis in fact), indirectly brings up a key point in relation to psychedelic experience with respect to the 'set' aspect of set and setting. if one has more experience with one class over the other, then it seems LSD would probably most closely resemble that class (in a general sense).
I completely agree with the idea that LSD cannot truly be called either a tryptamine or a phenethylamine. What really struck me about 69Ron's post is that I had always thought of LSD and friends as tryptamines. Likely this is because that is how Shulgin has traditionally classified them. I think it's really important to be clear that ergolines (or lysergamides if you please) are very distinctly different than either phenethylamines or tryptamines in their chemistry and pharmacology.

This entire 'science' of psychedelics is so much in its infancy that one cannot help but oversimplify. Shulgin himself is known to have said that at the start of his studies he considered there to be two classes of psychedelics, we all know which ones. However, after years of study and research, Shulgin entirely abandoned this notion for the idea that each psychedelic drug is unique in it's own sense and there really can't be any kind of true simplification due to the variety of differing effects on the very little understood human mind.


EDIT: Can we get all of this moved into an appropriate thread? I think there's some valuable information being presented and discussed.

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5-ht2a receptor, escaline, lsd, mescaline, mescaline effects, phenethylamine, psychedelic tolerance, psychedelics, tryptamine

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