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getting neurotransmitters to cross the bbb

^^^

Could there really be nearly enough NADH and CoQ10 to have significant therapeutic value as they seem to try to intimate are the actives responsible?

I would assume these other components are in very minor amopunts as well:
The leaves, seeds, stems and roots contain L-Dopa, Serotonin, 5-HTP, and Nicotine, as well as N,N-DMT, Bufotenine, and 5-MeO-DMT. It has a tradition of use as a Ayurvedic aphrodesiac, treatment for parkinsons, ayahuasca admixture, and coffee substitute.

This is interesting as well:

Phytother Res. 2004 Feb;18(2):97-101. Links
Effect of antiparkinson drug HP-200 (Mucuna pruriens) on the central monoaminergic neurotransmitters.Manyam BV, Dhanasekaran M, Hare TA.
Department of Neurology, Scott & White Clinic and Texas A & M University System Health Science Center College of Medicine, Temple, TX 76508, USA. [email protected]

HP-200, which contains Mucuna pruriens endocarp, has been shown to be effective in the treatment of Parkinson's disease. Mucuna pruriens endocarp has also been shown to be more effective compared to synthetic levodopa in an animal model of Parkinson's disease. The present study was designed to elucidate the long-term effect of Mucuna pruriens endocarp in HP-200 on monoaminergic neurotransmitters and its metabolite in various regions of the rat brain. HP-200 at a dose of 2.5, 5.0 or 10.0 g/kg/day was mixed with rat chow and fed daily ad lib to Sprague-Dawley rats (n = 6 for each group) for 52 weeks. Controls (n = 6) received no drug. Random assignment was made for doses and control. The rats were sacrificed at the end of 52 weeks and the neurotransmitters were analyzed in the cortex, hippocampus, substantia nigra and striatum. Oral administration of Mucuna pruriens endocarp in the form of HP-200 had a significant effect on dopamine content in the cortex with no significant effect on levodopa, norepinephrine or dopamine, serotonin, and their metabolites- HVA, DOPAC and 5-HIAA in the nigrostriatal tract. The failure of Mucuna pruriens endocarp to significantly affect dopamine metabolism in the striatonigral tract along with its ability to improve Parkinsonian symptoms in the 6-hydorxydopamine animal model and humans may suggest that its antiparkinson effect may be due to components other than levodopa or that it has an levodopa enhancing effect. Copyright 2004 John Wiley & Sons, Ltd. Copyright 2004 John Wiley & Sons, Ltd.

PMID: 15022157 [PubMed - indexed for MEDLINE]
 
I think the efficacy against parkinson's being better than pure l-dopa is becase M. pruriens has nicotine as well, and there are several studies that suggest that Nicotine helps with Parkinson's and Alzhiemer's.

btw, I recall reading somewhere that Fava beans (which are regularly eaten in non-western cultures) contain most of the same as M. pruriens.

Still though, I found both pure l-dopa and the extract to be as shitty as can be.
 
Is there really any substantial nicotine though as yes, indeed, nicotine and related agents have been shown to have such effects, but i again suspect levels are lower than therapeutic doses in any reasonable given amount of the herb

5Meo-DMT has been shown to be present at 0.0025%, 0.006% for DMT, both in the leaf and in same assay no note for nicotine

I believe the study showing the presence of nicotine was simply based on MY matches and has not been confirmed by a valid HPLC or the like...
 
hussness said:
Schizophrenia. I wasn't aware of a good animal model for drug testing.
Click to expand...

Oh, I understand your question now :) I'm not sure how much chronic high-dose L-DOPA treatment has been explored as an animal model of psychosis. However, clinical observations of Parkinsonian patients (especially those who use L-DOPA compulsively) provide a solid basis for the claim that taking L-DOPA in an uncontrolled manner can lead to psychotic symptoms.
 
How do i get GABA to cross the BBB? Just take stupid amounts?
Does L-Methinone cross at all?
 
Serotonin, Dopamine or Norepinephrine would just feel horrible if they crossed the BBB I think....

Splatt said:
How do i get GABA to cross the BBB? Just take stupid amounts?
Click to expand...

I think GABA is the only neurotransmitter that could be fun if it could cross the BBB...

But as you said you have to take huge amounts (grams), and even then, I don't think the effects are smuch stroger than placebo...

The russians (I think) had the idea to bind Niacin to GABA to make it cross the BBB, and it works, it's called Picamilon.....
 
5-HT2 said:
Oh, I understand your question now :) I'm not sure how much chronic high-dose L-DOPA treatment has been explored as an animal model of psychosis. However, clinical observations of Parkinsonian patients (especially those who use L-DOPA compulsively) provide a solid basis for the claim that taking L-DOPA in an uncontrolled manner can lead to psychotic symptoms.
Click to expand...
Bingo. I am also unaware of any animal studies that try to reporoduce this effect, but there are enough case reports of patients with parkinson's that have been given too high doses of L-DOPA and subsequently develop schizophrenic like symptoms that this idea should be contradicted for the average kid out there just looking to get fuxx0rred on neur0tranzmitterz.
 
i do not think as well the potential is there to get similar effects to the "beloved" dopaminergic drugs (cocaine, amphs, et al) simply by taking an acute dose of L-Dopa, potential side effect withstanding

in a carefully constructed cocktial or as an adjunctive agent it may enliven said effects, but as a standalone I do not think it will do the trick no matter what dose
 
jasoncrest said:
The russians (I think) had the idea to bind Niacin to GABA to make it cross the BBB, and it works, it's called Picamilon.....
Click to expand...
Picamilon works alright (though its effect is weaker than even gabapentin), but it had some strange effects enough to make me just not want to deal with it anymore. Its hard to describe these effects because they are more on the cognitive side. But there was also an issue in terms of physiology where picamilon seemed to have cused me a mild case of serotonin syndrome after taking it with 5-HTP.

I never touched either of those since then.
 
being a GABA thread and also above bringing up GHB, just curious if anyone has thoughts on GABOB and Baclofen stack...perhaps somewhat equatable to GHB?

both are not sched i believe anywhere....but mostly just curious from a scientific perspective of course =D
 
^ I have not tried GABOB, although very intregued about it, although from its structure and descriptions I read it seems to be no more powerful than phenibut or pregabalin.

As for Baclofen.. well, it really is just a muscle relaxant. Then again, I've never taken large enough doses of it.

The problem with trying to recreate the GHB experience with other drugs is that the GHB euphoria seems to come from those ubiquitous "GHB receptors", in addition to GABA-b agonism. While most of these GABA analogues fulfil the 2nd criterion, it seems that only a few (all illegal to my knowledge) compounds are active at the GHB receptor site.

Of course, I could be wrong...
 
Jamshyd said:
^ which is touted as being harmless yet curiously exasperates protracted GHB withdrawal even years after the habit was ended...
Click to expand...


hmm pleasse explain im interested

About to take 8 grams of it to goto bed and theres 3 grams of GABA under my tongue as I type, and Ive just eaten 300mg L-theaine
 
Jamshyd said:
^ I have not tried GABOB, although very intregued about it, although from its structure and descriptions I read it seems to be no more powerful than phenibut or pregabalin.

As for Baclofen.. well, it really is just a muscle relaxant. Then again, I've never taken large enough doses of it.

The problem with trying to recreate the GHB experience with other drugs is that the GHB euphoria seems to come from those ubiquitous "GHB receptors", in addition to GABA-b agonism. While most of these GABA analogues fulfil the 2nd criterion, it seems that only a few (all illegal to my knowledge) compounds are active at the GHB receptor site.

Of course, I could be wrong...
Click to expand...


OK, let's add in Trans-gamma-hydroxycrotonate for GHB-R agonism =D
 
Jamshyd said:
The problem with trying to recreate the GHB experience with other drugs is that the GHB euphoria seems to come from those ubiquitous "GHB receptors", in addition to GABA-b agonism. While most of these GABA analogues fulfil the 2nd criterion, it seems that only a few (all illegal to my knowledge) compounds are active at the GHB receptor site.

Of course, I could be wrong...
Click to expand...

IIRC...
Many of the developed GHB analogues such as t-HCA and GHV have greater affinity to GHB receptors than GHB itself, but lower affinity to GABA-B receptors than GHB, and I believe this is the reason they are reportedly less fun.

So the 'GHB experience' must have more behind it, or there is some sort of synergy going on between GABA receptors and GHB receptors..
There's also that 'dopamine build up effect' which I don't have much knowledge about.
 
I don't know any other way to get chemicals into brain that would't otherwise go, than using P-glycoprotein inhibitors. They are easy to find, for example black pepper and garlic contain them. 2g of black pepper contains enough for a dose according to one study.

P-glycoprotein Modulation: http://www.medscape.com/viewarticle/409741_2
 
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bigmac74 said:
IIRC...
Many of the developed GHB analogues such as t-HCA and GHV have greater affinity to GHB receptors than GHB itself, but lower affinity to GABA-B receptors than GHB, and I believe this is the reason they are reportedly less fun.

So the 'GHB experience' must have more behind it, or there is some sort of synergy going on between GABA receptors and GHB receptors..
There's also that 'dopamine build up effect' which I don't have much knowledge about.
Click to expand...

it may be interesting as such to see if one can hit on the right mix of say Baclofen (GABA-B) and THCA (GHB)...just the right amount and ratio may get pretty close or i guess simply reveal that there is definitely more going on with GHB if not so
 
<<How do i get GABA to cross the BBB? Just take stupid amounts?>>

A small percentage of GABA does cross the BBB, so this may work, although could have unhealty side effects. Valerian root contains a significant content of GABA, and is highly sedating, though it may contain other chemicals that cross the BBB or aid in the GABA crossing the BBB.
 
Jamshyd said:
Picamilon works alright (though its effect is weaker than even gabapentin), but it had some strange effects enough to make me just not want to deal with it anymore. Its hard to describe these effects because they are more on the cognitive side. But there was also an issue in terms of physiology where picamilon seemed to have cused me a mild case of serotonin syndrome after taking it with 5-HTP.

I never touched either of those since then.
Click to expand...

It works completely differently from Gabapentin though doesn't it? Or maybe not as much as I thought.
 
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