GHRP-2 / Ghrelin antagonist --> HGH benefits?

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    GHRP-2 / Ghrelin antagonist --> HGH benefits?


    Hi everybody.

    I did a injection of 300mcg GHRP-2 yesterday.
    first in the morning, second in the afternoon and
    the last directly after workout.
    GHRP should be 4-6 times stronger than ghrp 6.

    Well the hunger is incredible ! And i also got a very nice
    pump !! But what makes me unsure is:

    Well Ghrelin will support HGH release but ...
    Ghrelin does also stops your lipolysis ! So some
    benefits are shut down. Grhelin is also a factor for adiposity.

    GHRP-2 is an Ghrelin antagonist. An increased Ghrelin level
    makes you hungry but it lowers diretly after eating..
    But as an Antagonist, ghrp-2 will not decrease this level
    and left you hungry the whole time. Well if you have discipline, this should not be a problem.

    So if you think GHRP works better or in a different way
    and have some people here more experience in using this stuff ?

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    afaik ghrp2 is not 4-6 times stronger than ghrp6, in fact ghrp6 is superior though not hugely.
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    Quote Originally Posted by GBeefy View Post
    Hi everybody.

    I did a injection of 300mcg GHRP-2 yesterday.
    first in the morning, second in the afternoon and
    the last directly after workout.
    GHRP should be 4-6 times stronger than ghrp 6.

    Well the hunger is incredible ! And i also got a very nice
    pump !! But what makes me unsure is:

    Well Ghrelin will support HGH release but ...
    Ghrelin does also stops your lipolysis ! So some
    benefits are shut down. Grhelin is also a factor for adiposity.

    GHRP-2 is an Ghrelin antagonist. An increased Ghrelin level
    makes you hungry but it lowers diretly after eating..
    But as an Antagonist, ghrp-2 will not decrease this level
    and left you hungry the whole time. Well if you have discipline, this should not be a problem.

    So if you think GHRP works better or in a different way
    and have some people here more experience in using this stuff ?


    Are you saying GHRP-2 inhibits fat burning?


    There is this product call Xentropin that is basically a GHRP-2 oral strip with some other ingredients i beleive. I was interested in it.
    •   
       

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    Quote Originally Posted by superone View Post
    Are you saying GHRP-2 inhibits fat burning?


    There is this product call Xentropin that is basically a GHRP-2 oral strip with some other ingredients i beleive. I was interested in it.

    dont. its is not orally bioavailable in high enough amounts for any of these products to work. you would need grams of the stuff orally.
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    Quote Originally Posted by pumbertot View Post
    dont. its is not orally bioavailable in high enough amounts for any of these products to work. you would need grams of the stuff orally.

    So this stuff is a scam? Do you have any research that says it isnt orally bioavailable, even in their strip technology?


    Its funny that the only 2 posters on this site that say it works for them and 1 guy showed his before and after IGF-1 levels, as almost doubling, only have 1 or 2 posts lol, so it makes you wonder!
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    Quote Originally Posted by superone View Post
    So this stuff is a scam? Do you have any research that says it isnt orally bioavailable, even in their strip technology?


    Its funny that the only 2 posters on this site that say it works for them and 1 guy showed his before and after IGF-1 levels, as almost doubling, only have 1 or 2 posts lol, so it makes you wonder!
    pretty much, yes. this research has been shown before by datbtrue when someone else raised the issue. will try to find that.
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    wish that the tropins were still around.... that was DEF an orally active carrier.
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    Quote Originally Posted by superone View Post
    So this stuff is a scam? Do you have any research that says it isnt orally bioavailable, even in their strip technology?


    Its funny that the only 2 posters on this site that say it works for them and 1 guy showed his before and after IGF-1 levels, as almost doubling, only have 1 or 2 posts lol, so it makes you wonder!
    Hemogex...the real thing?
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    Quote Originally Posted by datBtrue View Post
    Dat... I see you state time and time again that GHS/GHRP not orally bio available (which with the studies provided and the product in question I def believe)

    BUT what was your take on the tropins that were out a lil while ago? They most definitely worked(and cost multiples of what this joke did) and worked for guys that were fairly experienced with these peptides in injectable form already. I see you talk about the one MK-0677 that is highly orally available but what again where the tropins??? do you know?

    As far as I remember they were just a special delivery matrix... given it was licensed by a pharm comp to IBE is it possible its the same MK-0677 you mentioned or something diff? if so why do you suppose more companies havnt taken a stab at a similar delivery matrix?
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    Quote Originally Posted by poopypants View Post
    Dat... I see you state time and time again that GHS/GHRP not orally bio available (which with the studies provided and the product in question I def believe)

    BUT what was your take on the tropins that were out a lil while ago? They most definitely worked(and cost multiples of what this joke did) and worked for guys that were fairly experienced with these peptides in injectable form already. I see you talk about the one MK-0677 that is highly orally available but what again where the tropins??? do you know?

    As far as I remember they were just a special delivery matrix... given it was licensed by a pharm comp to IBE is it possible its the same MK-0677 you mentioned or something diff? if so why do you suppose more companies havnt taken a stab at a similar delivery matrix?
    I remember that drug delivery system liscensed to IBE somehow temporaily changed the interoral mucosa lining, allowing transport into the blood stream, avoid the GI tract all together. Since the GI is where the peptides where destroyed. The tropins were great for me. If I remember correctly, that delivery system was being researched a viable alternative for insulin.

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    Quote Originally Posted by poopypants View Post
    As far as I remember they were just a special delivery matrix... given it was licensed by a pharm comp to IBE is it possible its the same MK-0677 you mentioned or something diff? if so why do you suppose more companies havnt taken a stab at a similar delivery matrix?
    Nonpeptidyl mimetics are developed and studied. MK-0677 was derived from GHRP-6 and developed by Merk. This entire process enabled modeling of the never before seen GHR and led to the eventual discovery of the native ligand.

    Nonpeptidyl mimetics have been developed & are currently being investigated that are derivatives of the GHRP Ipamorelin...

    There is no need to try to come up with a delivery system because these compounds are small molecules NOT lengthy amino acid chains. They are bioavailable.

    You can go read Roy G. Smith's long but detailed account on their development in Development of Growth Hormone Secretagogues, Endocrine Reviews 26 (3): 346-360

    Upon investigating its mechanism of action, we determined that GHRP-6 appeared to act through a novel receptor. Its activity was not blocked by the opiate receptor antagonist naloxone; furthermore, it was not a GHRH receptor agonist or a somatostatin receptor (sst) antagonist. Subsequently, my laboratory showed that GHRP-6 had two very important properties that made it an ideal prototype for the design of small molecules that would increase the amplitude of endogenous GH pulsatility; remarkably, in pituitary cells GHRP-6 amplified the GHRH signal transduction pathway and behaved as a functional antagonist of somatostatin.

    We sought a drug candidate with high oral bioavailability and pharmacokinetics suitable for once daily administration. Although GHRP-6 itself had properties consistent with an amplifier of GH release, GHRP-6 had poor oral bioavailability (0.3%) and short in vivo half-life (20 min) in humans (29). Furthermore, as a peptide it did not readily lend itself to optimization of pharmacokinetic properties by medicinal chemistry. Hence, GHRP-6 was selected only as a model structure; our objective was to design a nonpeptide mimetic. The probability of identifying a nonpeptide mimetic of GHRH was considered low because native GHRH is a 44-amino acid peptide, and the smallest known homolog to exhibit biological activity was a 29-mer.

    The GHRP-6 template also seemed ideal because it had been demonstrated that nonpeptide antagonists of small peptides could be designed based on a benzodiazepine template. However, an issue to be overcome at this time (1989) was the perceived difficulty of designing nonpeptide agonist mimetics. Fortunately, despite considerable resistance from some quarters, with the help of a few enthusiastic medicinal chemists, our efforts met with early success. Indeed, the design of GHRP-6 mimetics was considered a milestone achievement, because once we showed that such nonpeptide mimetics could be made, many more examples were forthcoming. For example, nonpeptide agonists of the peptides cholecystokinin, angiotensin, somatostatin, and melanocortin were developed.
    ...
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    sweet! so where are all these mimetics?

    Are they only available as DRUGS through pharms??
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    Quote Originally Posted by poopypants View Post
    sweet! so where are all these mimetics?

    Are they only available as DRUGS through pharms??
    I'm not going to cut and paste.

    You can read the section from my Growth Hormone Secretagogues article entitled:

    "Why you need both GHRH analog (CJC-1295) and GHRP"

    "GHS Down Regulation"

    ...post #3 in this thread: http://anabolicminds.com/forum/igf-1...dat-s-cjc.html
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    I thought this was an interesting article on an oral GHS. I know there was talk in here about orals either not working (OTC stuff) or products that once were available and now are not.


    Pharmacokinetics and Pharmacodynamic Effects of an Oral Ghrelin Agonist in Healthy Subjects

    Source: (Full free text): Pharmacokinetics and Pharmacodynamic Effects of an Oral Ghrelin Agonist in Healthy Subjects -- Piccoli et al. 92 (5): 1814 -- Journal of Clinical Endocrinology & Metabolism

    May 2007

    The Journal of Clinical Endocrinology & Metabolism Vol. 92, No. 5 1814-1820

    Abstract

    Context: An oral formulation of EP01572, a peptidomimetic growth hormone secretagogue, was studied. An oral delivery system would be preferable in many of the possible therapeutic indications of ghrelin agonists such as EP01572.

    Objectives: Our objective was to establish the pharmacological profile and the GH-releasing activity of increasing oral doses of EP01572 in healthy volunteers. In addition, the pharmacokinetics and pharmacological effects of EP01572 were investigated after intraduodenal (ID) administration.

    Setting: This study was a single-center escalating dose study with oral and ID applications.

    Subjects and Methods: In the first part, EP01572 was given orally to 36 male subjects; the treatment consisted of one oral dose of either EP01572 or placebo (0.005, 0.05, and 0.5 mg/kg body weight). Six subjects received two additional oral doses of EP01572: 0.125 and 0.25 mg/kg body weight. In the second part, the following treatments were performed in a randomized order: 1) administration of a bolus of saline (placebo) to the small intestine; 2) ID administration of a bolus of EP01572 at 0.2 mg/kg body weight; 3) ID perfusion of a bolus of EP01572 at 0.35 mg/kg body weight; and 4) ID perfusion of a bolus of EP01572 at 0.5 mg/kg body weight.

    Results: The oral and ID administration of EP01572 induced a rapid and dose-dependent increase in plasma drug concentrations and a potent GH release in healthy male volunteers.

    The following hormonal responses were statistically compared for potential differences using ANOVA on AUCs and maximal concentrations of the respective hormone. At higher doses, EP01572 marginally increased circulating levels of prolactin, with the biggest response seen at the highest dose (Fig. 5C), but ACTH and cortisol levels were not significantly changed (Fig. 5, A and B). EP01572 did not significantly alter plasma concentrations of glucose and insulin (Fig. 6 - Not shown here) or ghrelin levels (data not shown). All these hormonal parameters remained unchanged during placebo administration.

    FIG. 5. A, Effect of different doses of oral EP01572 on ACTH secretion over baseline. Data represent means SEM. B, Effect of different doses of oral EP01572 on cortisol secretion over baseline. Data represent means SEM. C, Effect of different doses of oral EP01572 on prolactin secretion over baseline. Data represent means SEM.


    The figure below is for GH release using ORALLY administered EP01572



    Conclusions: This study showed that EP01572 was active with regard to stimulation of GH release in humans after oral and ID administration
    Attached Images Attached Images  
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    Quote Originally Posted by papapumpsd View Post
    I thought this was an interesting article on an oral GHS. I know there was talk in here about orals either not working (OTC stuff) or products that once were available and now are not.
    No there was no question Papa.

    Yes GHRPs and their mimetics are orally active. But look at the dosing levels 25 - 50 grams!

    Twenty-five to fifty grams to achieve what 100 micro-grams will achieve if injected.

    Sure you get an increase in GH but after a few weeks you become desensitized.



    But even IF you didn't become desensitized you won't build a lot of tissue/muscle w/ any Ghrelin-mimetic because IGF-1 levels either are not elevated or the elevation is not sustained.

    The more interesting studies are the ones that give these things to short-stature children or GHD children over a period of time with the end result little or no growth.
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    Quote Originally Posted by datBtrue View Post
    No there was no question Papa.

    Yes GHRPs and their mimetics are orally active. But look at the dosing levels 25 - 50 grams! Yep
    Twenty-five to fifty grams to achieve what 100 micro-grams will achieve if injected.

    Sure you get an increase in GH but after a few weeks you become desensitized.

    But even IF you didn't become desensitized you won't build a lot of tissue/muscle w/ any Ghrelin-mimetic because IGF-1 levels either are not elevated or the elevation is not sustained.


    The more interesting studies are the ones that give these things to short-stature children or GHD children over a period of time with the end result little or no growth.
    Why is that interesting?? Interesting because GH is supposedly released due to the mimetic yet there is little to no growth? Or?

    I was also interested in the Prolactin & Cortisol graphs in relation to mimetic/GH dosing. That's why I squeezed them in there. I guess more for my benefit because I was interested in how they might be affecting me & my GHRH/GHRP protocol. (unrelated to bioavailability of oral mimetics)

    You did know that making a 50g shake of this mimetic would be a nice protein shake and boost GH? The GH shake It's for the Hollywood-types who don't like injections.
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    Quote Originally Posted by papapumpsd View Post
    Why is that interesting?? Interesting because GH is supposedly released due to the mimetic yet there is little to no growth? Or?
    Because that differs from giving someone a pill and then measuring GH over 24 hours or 3 day or 5 days.

    In those studies I find interesting a pill was given for many months with not much growth....that tells us a lot. Whereas the "one-off" studies tell us very little.

    Quote Originally Posted by papapumpsd;
    I was also interested in the Prolactin & Cortisol graphs in relation to mimetic/GH dosing. That's why I squeezed them in there. I guess more for my benefit because I was interested in how they might be affecting me & my GHRH/GHRP protocol. (unrelated to bioavailability of oral mimetics)

    You did know that making a 50g shake of this mimetic would be a nice protein shake and boost GH? The GH shake It's for the Hollywood-types who don't like injections.
    Not directed at you my man. You're one of my favorite peeps for sure.

    No I am a little sensitive about all of this because a board sponsor puts out and is planning on even a newer oral "GHS" product.

    In my opinion they (LegalGear) don't know what they are talking about. I have no problem with them making money or their customer base being ignorant. I'm just allergic to mendacity...thats all.
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    Quote Originally Posted by datBtrue View Post
    Because that differs from giving someone a pill and then measuring GH over 24 hours or 3 day or 5 days.

    In those studies I find interesting a pill was given for many months with not much growth....that tells us a lot. Whereas the "one-off" studies tell us very little.



    Not directed at you my man. You're one of my favorite peeps for sure.

    No I am a little sensitive about all of this because a board sponsor puts out and is planning on even a newer oral "GHS" product.

    In my opinion they (LegalGear) don't know what they are talking about. I have no problem with them making money or their customer base being ignorant. I'm just allergic to mendacity...thats all.
    Hey, you can only blame yourself for ignorance, especially when buying retail products. I read reviews on products before I buy and I also read up on them too (this includes sports supplements and "experimental" supps.).

    I hear you man!
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    Is the peptide being broken down in the stomach or is the small intestine just inefficient at absorption? Could a coated pill cause a greater increase in oral efficiency?
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    Quote Originally Posted by java568 View Post
    Is the peptide being broken down in the stomach or is the small intestine just inefficient at absorption? Could a coated pill cause a greater increase in oral efficiency?
    Java, read the study I posted above (the free full text link). They have data on interduodenal administration as well.
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    Quote Originally Posted by papapumpsd View Post
    Java, read the study I posted above (the free full text link). They have data on interduodenal administration as well.
    haha wow thanks dunno how I missed that it was ID
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    Does anyone have any information on a woman taking Xentropin. I had a doctor mention administering it to me through Bio Identical Hormone Replacement thearpy. He said it is an oral form. How do I know if it is legit?

    ~Justine
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    Quote Originally Posted by datBtrue View Post
    hemogex
    Though this might be anecdotal, I've tried both Hexatropin and Hemogex. Hexatropin was by far superior. I know the content is different though.
  

  
 

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