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powerfull vs Bulk 1-carboxy-2-amino-3-pyrobenzo

  1.  09-05-2007  01:05 PM
    Featured Author Patrick Arnold's Avatar
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    Originally Posted by Dr. Gonzo View Post
    Pat, as sketchy as this stuff seems, and I do sympathize with all of your sentiments...1-Carboxy is not the same as L-Dopa.
    It isn't?

    please explain the chemical differences. what IS the stuff then if it is not L-dopa?

    a real chemical name would be nice.



  2.  09-05-2007  01:20 PM
    Recovering AXoholic thesinner's Avatar
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    Originally Posted by Patrick Arnold View Post
    It isn't?

    please explain the chemical differences. what IS the stuff then if it is not L-dopa?

    a real chemical name would be nice.
    I've been wondering this myself for quite some time, as well.
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  3.  09-05-2007  01:40 PM
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    Originally Posted by thesinner View Post
    I've been wondering this myself for quite some time, as well.

    pyrobenzol is an archaic alternative name for benzene so breaking the name down it appears that it either is a screwed up name for L-dopa or it is sort of a butanoic acid derivative of l-dopa (which has a propionic acid side chain). but if it is the latter then it would not be a dopamine precursor at all

    I think they tried to be fancy with the name and messed up. what they should have said (and not that the structure of the name is right anyway) was

    2-carboxy-2-amino-1-pyrobenzol-(3,4-diol)


    bottom line is, this is not a derivative of L-dopa. It is just L-dopa plain and simple

  4.  09-05-2007  01:53 PM
    Registered User ReaperX's Avatar
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    Originally Posted by Patrick Arnold View Post
    pyrobenzol is an archaic alternative name for benzene so breaking the name down it appears that it either is a screwed up name for L-dopa or it is sort of a butanoic acid derivative of l-dopa (which has a propionic acid side chain). but if it is the latter then it would not be a dopamine precursor at all

    I think they tried to be fancy with the name and messed up. what they should have said (and not that the structure of the name is right anyway) was

    2-carboxy-2-amino-1-pyrobenzol-(3,4-diol)


    bottom line is, this is not a derivative of L-dopa. It is just L-dopa plain and simple

    Isn't a typo in the ingredients for a product fall under 'mislabeling' supplements and illegal ? Even if it is a typo it is not exactly the name of the ingredient. While 99.9% of the IUPAC nomenclature is correct, we all know a number,dash,bond location, etc makes a world difference, but by law, supplements need to have accurate labeling of their products ?

  5.  09-05-2007  01:53 PM
    Registered User xjsynx's Avatar
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    I wasn't impressed with PowerFULL, and USP wasn't impressed with me for saying so...

  6.  09-05-2007  01:57 PM
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    Originally Posted by xjsynx View Post
    I wasn't impressed with PowerFULL, and USP wasn't impressed with me for saying so...
    you know what ? I wasn't impressed with anabolic pump either. go figure.

  7.  09-05-2007  02:01 PM
    Featured Author Patrick Arnold's Avatar
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    test test

  8.  09-05-2007  02:04 PM
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    Originally Posted by ReaperX View Post
    Isn't a typo in the ingredients for a product fall under 'mislabeling' supplements and illegal ? Even if it is a typo it is not exactly the name of the ingredient. While 99.9% of the IUPAC nomenclature is correct, we all know a number,dash,bond location, etc makes a world difference, but by law, supplements need to have accurate labeling of their products ?
    Yes you are correct, also companies are required under the FTC guidelines to list the common name of a product on the ingredient panel, not some obscure chemical name.

  9.  09-05-2007  02:11 PM
    Registered User xjsynx's Avatar
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    Originally Posted by Patrick Arnold View Post
    usp, apn, and controlled labs all seem eerily the same to me.

    the same as in the way they come across on the internet.

    everything they have is amazing, mindblowind, incredible. all this feedback all the time

    then you have other well known companies with fantastic products but you don't see nearly as much talk about the products (i am not talking about ergo either)

    i dunno, i am just thinking out loud.
    For the most part marketing and being part of the 'inner circle'.

  10.  09-05-2007  02:12 PM
    Registered User Dr. Gonzo's Avatar
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    Uh-oh...

    Maybe they weren't so far off about that BBB thing:

    1: Exp Neurol. 2005 Sep;195(1):267-71. Links
    An active transport system in the blood-brain barrier may reduce levodopa availability.Hawkins RA, Mokashi A, Simpson IA.


    Levodopa, the primary drug used to treat patients with Parkinson's disease, is transported into the brain by the facilitative amino acid transporter (L1). We present here an unanticipated discovery: levodopa may be pumped out of the brain by a Na(+)-dependent transport system that couples the naturally occurring Na(+) gradient existing between the brain's extracellular fluid and the cytoplasm of capillary endothelial cells. The activity of this system reduces the net availability of levodopa.

  11.  09-05-2007  02:15 PM
    Featured Author Patrick Arnold's Avatar
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    Originally Posted by Dr. Gonzo View Post
    Uh-oh...

    Maybe they weren't so far off about that BBB thing:

    1: Exp Neurol. 2005 Sep;195(1):267-71. Links
    An active transport system in the blood-brain barrier may reduce levodopa availability.Hawkins RA, Mokashi A, Simpson IA.


    Levodopa, the primary drug used to treat patients with Parkinson's disease, is transported into the brain by the facilitative amino acid transporter (L1). We present here an unanticipated discovery: levodopa may be pumped out of the brain by a Na(+)-dependent transport system that couples the naturally occurring Na(+) gradient existing between the brain's extracellular fluid and the cytoplasm of capillary endothelial cells. The activity of this system reduces the net availability of levodopa.

    maybe who wasn't so far off about what?

    L-dopa is a prodrug of dopamine that passess through the BBB. Anyone with half knowledge of pharmacology is quite familiar with this as it is one of the most famous drugs of the 20th century

  12.  09-05-2007  02:16 PM
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    Originally Posted by Patrick Arnold View Post
    pyrobenzol is an archaic alternative name for benzene so breaking the name down it appears that it either is a screwed up name for L-dopa or it is sort of a butanoic acid derivative of l-dopa (which has a propionic acid side chain). but if it is the latter then it would not be a dopamine precursor at all

    I think they tried to be fancy with the name and messed up. what they should have said (and not that the structure of the name is right anyway) was

    2-carboxy-2-amino-1-pyrobenzol-(3,4-diol)


    bottom line is, this is not a derivative of L-dopa. It is just L-dopa plain and simple
    I understand where you're coming from here, but based on the totally different subjective effects...I would be surprised.

    Unless my brain chemistry has changed since using the L-dopa, and I'm handling the same compound differently...which I suppose could be the case with what goes in and out of my brain on a daily basis.

  13.  09-05-2007  02:35 PM
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    Originally Posted by Patrick Arnold View Post
    maybe who wasn't so far off about what?

    L-dopa is a prodrug of dopamine that passess through the BBB. Anyone with half knowledge of pharmacology is quite familiar with this as it is one of the most famous drugs of the 20th century
    Right, but the above study is demonstrating a problem with L-Dopa's sustained central bioavailibility. To say that it doesn't cross the BBB is wrong, however. I'm saying this is probably where USP got the idea to claim that it doesn't cross the BBB.

    This study is interesting to, from July of '07:

    : Pharm Res. 2007 Jul;24(7):1309-24. Epub 2007 Apr 3. Links
    Novel L-Dopa and dopamine prodrugs containing a 2-phenyl-imidazopyridine moiety.Denora N, Laquintana V, Lopedota A, Serra M, Dazzi L, Biggio G, Pal D, Mitra AK, Latrofa A, Trapani G, Liso G.


    PURPOSE: The aim of this study was to gain insight into the feasibility of enhancing the delivery of L-Dopa and dopamine to the brain by linking these neurotransmitters and L-Dopa ethyl ester to 2-phenyl-3-carboxymethyl-imidazopyridine compounds giving rise to the so-called Dopimid compounds. MATERIALS AND METHODS: A number of Dopimid compounds were synthesized and both stability and binding studies to dopaminergic and benzodiazepine receptors were performed. To evaluate whether Dopimid compounds are P-gp substrates, [(3)H]ritonavir uptake experiments and bi-directional transport studies on confluent MDCKII-MDR1 monolayers were carried out. The brain penetration properties of Dopimid compounds were estimated by the Clark's computational model and evaluated by investigation of their transport across BBMECs monolayers. The dopamine levels following the intraperitoneal administration of the selected Dopimid compounds were measured in vivo by using brain microdialysis in rat. RESULTS: Tested compounds were adequately stable in solution buffered at pH 7.4 but undergo faster cleavage in dilute rat serum at 37 degrees C. Receptor binding studies showed that Dopimid compounds are essentially devoid of affinity for dopaminergic and benzodiazepine receptors. [(3)H]ritonavir uptake experiments indicated that selected Dopimid compounds, like L-Dopa and dopamine hydrochloride, are not substrates of P-gp and it was also confirmed by bi-directional transport experiments across MDCKII-MDR1 monolayers. By Clark's model a significant brain penetration was deduced for L-Dopa ethyl ester and dopamine derivatives. Transport studies involving BBMECs monolayers indicated that some of these compounds should be able to cross the BBB. Interestingly, the rank order of apparent permeability (P (app)) values observed in these assays parallels that calculated by the computational approach. Brain microdialysis experiments in rat showed that intraperitoneal acute administration of some Dopimid compounds induced a dose-dependent increase in cortical dopamine output. CONCLUSION: Based on these results, it may be concluded that some Dopimid compounds can be proposed as novel L-Dopa and dopamine prodrugs.

    PMID: 17404814 [PubMed - indexed for MEDLINE]

  14.  09-05-2007  03:43 PM
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    Originally Posted by Dr. Gonzo View Post
    Right, but the above study is demonstrating a problem with L-Dopa's sustained central bioavailibility. To say that it doesn't cross the BBB is wrong, however. I'm saying this is probably where USP got the idea to claim that it doesn't cross the BBB.

    This study is interesting to, from July of '07:

    : Pharm Res. 2007 Jul;24(7):1309-24. Epub 2007 Apr 3. Links
    Novel L-Dopa and dopamine prodrugs containing a 2-phenyl-imidazopyridine moiety.Denora N, Laquintana V, Lopedota A, Serra M, Dazzi L, Biggio G, Pal D, Mitra AK, Latrofa A, Trapani G, Liso G.


    PURPOSE: The aim of this study was to gain insight into the feasibility of enhancing the delivery of L-Dopa and dopamine to the brain by linking these neurotransmitters and L-Dopa ethyl ester to 2-phenyl-3-carboxymethyl-imidazopyridine compounds giving rise to the so-called Dopimid compounds. MATERIALS AND METHODS: A number of Dopimid compounds were synthesized and both stability and binding studies to dopaminergic and benzodiazepine receptors were performed. To evaluate whether Dopimid compounds are P-gp substrates, [(3)H]ritonavir uptake experiments and bi-directional transport studies on confluent MDCKII-MDR1 monolayers were carried out. The brain penetration properties of Dopimid compounds were estimated by the Clark's computational model and evaluated by investigation of their transport across BBMECs monolayers. The dopamine levels following the intraperitoneal administration of the selected Dopimid compounds were measured in vivo by using brain microdialysis in rat. RESULTS: Tested compounds were adequately stable in solution buffered at pH 7.4 but undergo faster cleavage in dilute rat serum at 37 degrees C. Receptor binding studies showed that Dopimid compounds are essentially devoid of affinity for dopaminergic and benzodiazepine receptors. [(3)H]ritonavir uptake experiments indicated that selected Dopimid compounds, like L-Dopa and dopamine hydrochloride, are not substrates of P-gp and it was also confirmed by bi-directional transport experiments across MDCKII-MDR1 monolayers. By Clark's model a significant brain penetration was deduced for L-Dopa ethyl ester and dopamine derivatives. Transport studies involving BBMECs monolayers indicated that some of these compounds should be able to cross the BBB. Interestingly, the rank order of apparent permeability (P (app)) values observed in these assays parallels that calculated by the computational approach. Brain microdialysis experiments in rat showed that intraperitoneal acute administration of some Dopimid compounds induced a dose-dependent increase in cortical dopamine output. CONCLUSION: Based on these results, it may be concluded that some Dopimid compounds can be proposed as novel L-Dopa and dopamine prodrugs.

    PMID: 17404814 [PubMed - indexed for MEDLINE]

    whatever the case, they really threw me for a a "WTF?" by saying that L-dopa does not cross the blood brain barrier.

    certainly the derivative in the abstract there is too sophisticated and expensive for a supplement. and if you were gonna get that complex you are better served spending the resources and intellectual capital on more promising avenues then L-dopa

  15.  09-05-2007  04:10 PM
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    Originally Posted by Patrick Arnold View Post
    pyrobenzol is an archaic alternative name for benzene so breaking the name down it appears that it either is a screwed up name for L-dopa or it is sort of a butanoic acid derivative of l-dopa (which has a propionic acid side chain). but if it is the latter then it would not be a dopamine precursor at all

    I think they tried to be fancy with the name and messed up. what they should have said (and not that the structure of the name is right anyway) was

    2-carboxy-2-amino-1-pyrobenzol-(3,4-diol)


    bottom line is, this is not a derivative of L-dopa. It is just L-dopa plain and simple

    I never heard anyone say it was a precursor. Maybe it is, maybe it isn't, but I would imagine there could be other ways for it to raise dopamine levels. I've had suspicions about a few other products by USPLabs (ingredients with uncommon names), but I try to keep an open mind about it.

    Here's what they had on their writeup about 1-C, in case you hadn't seen it.

    A few years back a compound hit the bodybuilding scene with a lot of promise. It had great scientific research to back it up. That compound’s name was L-Dopa.

    As you may know, L-Dopa could never duplicate it’s scientific performance in the real world. For one reason: L-Dopa could never cross the blood brain barrier…it would get absorbed in the blood stream and all hope of increased HGH production was lost!

    In order for the brain to turn L-Dopa into dopamine…and therefore shoot HGH levels through the roof…this major obstacle had to be overcome…

    At USP Labs we knew if we could come up with a bioavailable form of L-Dopa that had the ability to cross the blood/brain barrier it would help bodybuilders everywhere increase natural HGH release, natural Testosterone production, drive sex drive through the roof, build muscle, lose body fat and sleep like a rock.

    Well, you will be glad when you hear we have succeeded! But, we totally skipped the L-Dopa part and discovered a brand new compound that’s closely related and is readily available for the body to use!

    It’s called 1-C and it’s here to rock your world…

    1-C, or 1-carboxy-2-amino-3-pyrobenzol(3,4 diol), is closely related to l-Dopa. In the past, many supplements touted L-Dopa as the next BIG THING in the supplement industry, but if failed miserably.

    Synthetic L-dopa was created by the pharmaceutical industry to use in Parkisons disease to increase Dopamine levels that could increase muscle coordination. The research was good and bad mainly because Parkisons is not a well understood disease yet.

    Again, in a study done in India, it was found that 1-C (a natural l-Dopa derivative) increased HGH levels through increasing dopamine levels naturally.
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  16.  09-05-2007  04:27 PM
    Featured Author Patrick Arnold's Avatar
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    Originally Posted by thesinner View Post
    I never heard anyone say it was a precursor. Maybe it is, maybe it isn't, but I would imagine there could be other ways for it to raise dopamine levels. I've had suspicions about a few other products by USPLabs (ingredients with uncommon names), but I try to keep an open mind about it.

    Here's what they had on their writeup about 1-C, in case you hadn't seen it.

    the herb they say this is from is the same herb that everyone else gets regular l-dopa from

    everything points to this being plain l-dopa

    i would love for them to prove me wrong

  17.  09-05-2007  04:40 PM
    Recovering AXoholic thesinner's Avatar
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    Originally Posted by Patrick Arnold View Post
    the herb they say this is from is the same herb that everyone else gets regular l-dopa from

    everything points to this being plain l-dopa

    i would love for them to prove me wrong
    Just because you know there's one particular alkaloid in the plant, doesn't mean that's the only one it contains. A lot of times plants contain several very similar alkaloids in them, look at chocolate, yerba mate, and guarana; they contain several xanthine group alkaloids in varying concetrations.
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  18.  09-05-2007  04:43 PM
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    Originally Posted by thesinner View Post
    Just because you know there's one particular alkaloid in the plant, doesn't mean that's the only one it contains. A lot of times plants contain several very similar alkaloids in them, look at chocolate, yerba mate, and guarana; they contain several xanthine group alkaloids in varying concetrations.

    i am aware of that

    but surely this would be a compound i would be familiar with, and others would be familiar with if it indeed is present in mucura puriens along with l-dopa

    you are a nice guy so why don't you enquire with usp about this. i hope they don't play the "propietary information" game

  19.  09-05-2007  04:46 PM
    Registered User xjsynx's Avatar
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    All this L-dopa talk makes me think of Leonard...


  20.  09-05-2007  04:51 PM
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    Originally Posted by Patrick Arnold View Post

    you are a nice guy so why don't you enquire with usp about this. i hope they don't play the "propietary information" game
    2nd that vote. I'd like to hear what they have to say.

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