Norcoclaurine HCl-Thoughts?

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    Norcoclaurine HCl-Thoughts?


    Norcoclaurine HCl (NorcolineTM) Effective as a stimulant or not?

    I've been seeing it a bit more in Supplements, wondering it's effectiveness, if any or if great, at all...Is it actually Beneficial or just an addendum in the hope of replacing DMAA...maybe just a Filler?

    Josh, Cyrus...Any articles or clearing up on this? I got some info myself, but I like the big boys educating us better before even throwing up whatever I have found !
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    It is an effective beta agonist. The downfall is an extremely short plasma halflife (~10 minutes). Finding a way to prolong it's HL would theoretically provide a pretty effective stimulant.
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    The above is my own opinion and does not reflect the opinion of PES
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    Quote Originally Posted by mr.cooper69
    It is an effective beta agonist. The downfall is an extremely short plasma halflife (~10 minutes). Finding a way to prolong it's HL would theoretically provide a pretty effective stimulant.
    That's what I wanted to hear. Effective, just short lived ATM...hm...thanks Cy!
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    Is this at all similar to Higenamine. All I see in pubmed when searching for norcoclaurine is that it is involved in opioid synthesis, which would be anything but a stimulatory....unless it reduces norcoclaurine synthase activity?
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    Quote Originally Posted by ZiR RED View Post
    Is this at all similar to Higenamine. All I see in pubmed when searching for norcoclaurine is that it is involved in opioid synthesis, which would be anything but a stimulatory....unless it reduces norcoclaurine synthase activity?
    It is higenamine HCl
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    Quote Originally Posted by ZiR RED
    Is this at all similar to Higenamine. All I see in pubmed when searching for norcoclaurine is that it is involved in opioid synthesis, which would be anything but a stimulatory....unless it reduces norcoclaurine synthase activity?
    Quote Originally Posted by mr.cooper69

    It is higenamine HCl
    That's what my initial search told me , it bounced back Higenamine and I thought I was wrong and didn't wanna appear stupid...what's the point of naming it differently and passing it as a novelty in certain products now then?
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    Quote Originally Posted by Celorza

    That's what my initial search told me , it bounced back Higenamine and I thought I was wrong and didn't wanna appear stupid...what's the point of naming it differently and passing it as a novelty in certain products now then?
    Ah...this isn't the place to name products, but there are many supps that will use different nomenclatures to confuse people. Especially chemical names to make things look steroidal(not referring to this ingredient).

    Edit: check out the Hightower pharmacology blog for a good write up. That blog is great.
    http://anabolicminds.com/forum/workout-logs/231713-rob112-3-means.html
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    Quote Originally Posted by rob112 View Post
    Ah...this isn't the place to name products, but there are many supps that will use different nomenclatures to confuse people. Especially chemical names to make things look steroidal(not referring to this ingredient).

    Edit: check out the Hightower pharmacology blog for a good write up. That blog is great.
    lol not naming products, I already know that website, and I read also databases of articles for research. I liked to point this out here for discussion of its effectiveness and possibly to show some wild and false claims I have seen on some product write ups about it.
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    Might be fun to take before a good romping session...

    Int J Impot Res. 2012 Mar-Apr;24(2):77-83. doi: 10.1038/ijir.2011.48. Epub 2011 Sep 29.
    The relaxation effect and mechanism of action of higenamine in the rat corpus cavernosum.

    Kam SC, Do JM, Choi JH, Jeon BT, Roh GS, Chang KC, Hyun JS.
    Source

    Department of Urology, Institute of Health Sciences, Gyeongsang National University School of Medicine, Jinju, Korea.

    Abstract

    Higenamine mediates cardiotonic, vascular relaxation and bronchodilator effects. The relaxation effects and the mechanism of action of higenamine on the rat corpus cavernosum (CC) were assessed to investigate the effect of higenamine on penile erection. Strips of CC and aorta were used in organ baths for isometric tension studies. Tension was measured with isometric force transducers, and muscle relaxation was expressed as the percent decrease in precontraction induced by phenylephrine (PE). The relaxation reactions were investigated in an endothelial-denuded group and groups pretreated with N(G)-nitro-L-arginine methyl ester (NO synthesis inhibitor), propranolol (β-receptor blocker), indomethacin (COX inhibitor), glibenclamide (K(+)(ATP) channel inhibitor), 4-aminopyridine (membrane potential-dependent potassium channel inhibitor) and methylene blue (guanylyl cyclase inhibitor) for 30 min. Intracavernous pressure (ICP) was assessed in rats after the intravenous administration of higenamine, and changes in guanosine 3',5'-cyclic monophosphate and adenosine 3',5'-cyclic monophosphate (cAMP) concentrations were measured on the basis of the higenamine concentration. Also, the combined reaction of higenamine and the phosphodiesterase type-5 (PDE-5) inhibitors was assessed. Higenamine induced relaxation of the CC and the aortic strips precontracted with PE in a dose-dependent manner. The CC was significantly more relaxed than the aortic rings in response to the same higenamine concentration (P<0.05). The CC relaxation reaction was suppressed by the β-receptor blocker propranolol. The cAMP concentration increased gradually with increased higenamine concentration (P<0.05). The ICP also increased with increased higenamine concentration in vivo (P<0.05). In the group pretreated with 10(-7) M higenamine, the relaxation reaction of CC induced by the PDE-5 inhibitor increased significantly, compared with CC exposed to the PDE-5 inhibitor but not pretreated with higenamine (P<0.05). In conclusion, higenamine induced relaxation of the rat CC in a dose-dependent manner. The effect may be mediated through β-adrenoceptors. The results suggest that higenamine may be valuable as a new lead compound for treating erectile dysfunction.

    PMID:21956762 [PubMed - indexed for MEDLINE]
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    Quote Originally Posted by mr.cooper69 View Post
    It is an effective beta agonist. The downfall is an extremely short plasma halflife (~10 minutes). Finding a way to prolong it's HL would theoretically provide a pretty effective stimulant.

    A couple of points that should be made.
    1. if higenamine has otheractive metabolites, then beneficial effects may continue to be seen aftercomplete elimination of the parent compound, depending upon thepharmacokinetics of those particular metabolites.

    2. Having said that, this 10 minute plasma half-life figure is not being usedcorrectly in the context of the higenamine in the products. Half-life can andis often dependent upon the route of administration and sometimes the dose. Itis a critical error to take any pharmacokinetic variable's result from oneroute of administration and apply it to another. The only way to know what theplasma half-life after oral administration is to evaluate the plasma half-lifeafter oral administration. You can't take the half-life after intravenousadministration and apply that to oral administration. Usually, the half-lifeafter oral administration will be longer than that seen after intravenous. But,there are times where they will be the same or where the intravenous route willactually result in a longer half-life (more the exception).

    3. If you use this stimulant, you'll understand half life is longer than 10 minutes.

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    1. This I agree with, and is the reason I believe I experience prolonged stimulation from higenamine, though I haven't really taken time to trace out its metabolites.

    2. Eh, the HL may be longer orally, but then you have to account for other variables like AUC of plasma concentrations, pharmacodynamic issues (which wouldn't quite manifest as strongly via IV ), bioavailability (forseeably around 3% or less vs the obviously high IV bioavailability) etc...Ultimately, the difference in HL from administration methods in this instance will likely not account for the prolonged stim effect.

    3. See #1
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    Personally my favorite stimulant...strong beta-agonist properties. The feel lasts 3-4 hours without a doubt. I feel it in the stimulation, the performance, and the breathing.
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    Quote Originally Posted by mr.cooper69 View Post
    1. This I agree with, and is the reason I believe I experience prolonged stimulation from higenamine, though I haven't really taken time to trace out its metabolites.

    2. Eh, the HL may be longer orally, but then you have to account for other variables like AUC of plasma concentrations, pharmacodynamic issues (which wouldn't quite manifest as strongly via IV ), bioavailability (forseeably around 3% or less vs the obviously high IV bioavailability) etc...Ultimately, the difference in HL from administration methods in this instance will likely not account for the prolonged stim effect.

    3. See #1

    wouldn't the AUC havealready been known and considered for the half-life ultimately to getcalculated? where did you get bioavailability to be 3% orless?
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    I've used Alpha T2, Jack3d Micro and currently Alphamine.

    All which contain Higenamine and all have given me great results in fat loss, energy and performance.
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    Quote Originally Posted by USPowders View Post
    wouldn't the AUC havealready been known and considered for the half-life ultimately to getcalculated? where did you get bioavailability to be 3% orless?
    The bioavailability in rabbits is 2-5%. Yes, the AUC would have to be known, but as with all agents, there is a therapeutic window of plasma concentrations at which the ingredient exerts its effects (for instance, caffeine may have a ~5 hour halflife but you certainly won't feel it in your system 10 hours later when 25% of the initial dose is still present). So, oral effects may not be in parallel with IV effects of the compound. Thankfully, there is data for both methods of administration and the bioavailability isn't limiting since norcoclaurine requires a low dose anyway, but certain effects demonstrated via IV simply cannot be extrapolated to oral dosing with such ease.
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