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Old 05-02-2008, 09:58 PM   #1
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Glycyrrhetinic acid (a topical fat loss ingredient)

So as I understand it, once this chemical is broken down into metabolites by the body, one of those metabolites helps keep
cortisol active, and encourages kidney build up? Can someone
help me understand why this is something a consumer would want in a cutting product?

Glycyrrhetinic acid - Wikipedia, the free encyclopedia

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The structure of glycyrrhetinic acid is similar to that of cortisone. Both molecules are flat and similar at position 3 and 11. This might be the basis for licorice's anti-inflammatory action.

3-Beta-D-(monoglucuronyl)18-beta-glycyrrhetinic acid, a metabolite of glycyrrhetinic acid inhibits the conversion of active cortisol to inactive cortisone in the kidneys. This occurs via inhibition of the enzyme by inhibiting the enzyme 11-beta-hydroxysteroid dehydrogenase. As a result, cortisol levels are high within the collecting duct of the kidney. Cortisol has intrinsic mineralocorticoid properties (that is, it acts like aldosterone and increases sodium reabsorption) that work on ENaC channels in the collecting duct. Hypertension develops due to this mechanism of sodium retention. People often have high blood pressure with a low renin and low aldosterone blood level. The increased amounts of cortisol binds to the unprotected, unspecific mineralocorticoid receptors and induce sodium and fluid retention, hypokalaemia, high blood pressure and inhibition of the renin-angiotensin-aldosterone system. Therefore licorice should not be given to patients with a known history of hypertension.



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Old 05-02-2008, 10:07 PM   #2
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I believe it works in topicals because they are not systematic, thus only inihibiting the conversion of cortisone to cortisol locally.
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Old 05-02-2008, 10:13 PM   #3
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Quote:
Originally Posted by thesinner
I believe it works in topicals because they are not systematic, thus only inihibiting the conversion of cortisone to cortisol locally.
but the article is quoted as saying it's the other way around, that it prevents the kidneys from deactivating cortisol through metabolism, So, unless the article got things mixed up, it would seem this chemical is actually a bad thing. Either that or it's a flaw of my understanding, is cortisol only undesirable when inactive?



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Old 05-02-2008, 11:57 PM   #4
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I believe there is a difference between kidney tissue and adipose tissue.

And there is a difference between systemic and local application.



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Old 05-03-2008, 02:05 AM   #5
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Quote:
Originally Posted by Sir Savage
I believe there is a difference between kidney tissue and adipose tissue.

And there is a difference between systemic and local application.
yes, but I wouldn't assume that just because you administer a chemical transdermally in a localized area that it would only affect certain tissues in certain areas. Otherwise, you wouldn't be able to drop say, liquid LSD for example under your tongue, in your eye, or in larger doses on the skin and not have it affect your brain. Venomous frogs that are lethal to the touch might be another good example of this. Besides, regardless of the limitations of topical mediums, it still doesn't give me any clue as to what benefits this ingredient would provide. In short, I'm merely asking 'what is its purpose in fat reduction, and how does it work?'
'



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Old 05-03-2008, 02:20 AM   #6
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Quote:
Originally Posted by Nightwanderer
yes, but I wouldn't assume that just because you administer a chemical transdermally in a localized area that it would only affect certain tissues in certain areas. Otherwise, you wouldn't be able to drop say, liquid LSD for example under your tongue, in your eye, or in larger doses on the skin and not have it affect your brain. Venomous frogs that are lethal to the touch might be another good example of this. Besides, regardless of the limitations of topical mediums, it still doesn't give me any clue as to what benefits this ingredient would provide. In short, I'm merely asking 'what is its purpose in fat reduction, and how does it work?'
'
Again, you are referring to systemic instead of localized. With GA locally applied in the carrier within Napalm, the majority of the actives stays in the applied area, thus reducing cortisol deposits.
FYI, localized carriers (e.g. the active in Napalm, Lipo-U) are used to apply supplements in a localized area. This metjod not only makes spot reduction possible, but also severely reduces the systemic effects of Y-HCl, etc. This is why adding clen to the carrier will not have the negative effects on VO2, BP, etc.



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Old 05-03-2008, 05:18 PM   #7
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Quote:
Originally Posted by Nightwanderer
but the article is quoted as saying it's the other way around, that it prevents the kidneys from deactivating cortisol through metabolism, So, unless the article got things mixed up, it would seem this chemical is actually a bad thing. Either that or it's a flaw of my understanding, is cortisol only undesirable when inactive?
GA lowers cortisol.

The text below,taken from the Napalm writeup,explains in detail how GA acts as a fat loss agent.


Glycyrrhetinic acid
Licorice has a lengthy historical association with reduction fat mass and weight loss dating back to the 4th century BC. The Greek physician Theophrastus noted that licorice root granted his patience 'freedom from hunger and thirst'(24), an observation that was reaffirmed in the 1st century BC by Plinius (25). It wasn't until modern technological advancements allowed us to characterize the licorice root in order to reveal the main active ingredient: glycyrrhetinic acid (GA).

These ancient observations are supported thoroughly by modern literature which documents the relationship between GA and 11?-hydroxysteroid dehydrogenase (11HSD) (26). For our purposes we will concern ourselves with the first of two 11HSD subtypes. 11HSD1 is found in subcutaneous adipocytes in a relatively lesser abundance than it's visceral counterpart (27). However, 11HSB-1 is sufficiently concentrated to perform its primary function and influence the level of cortisol by reactivating the inactive cortisone. A hyperactive mutant form of 11HSD-1 is observed in cases of the pathologically obese, suggesting that inhibition of this enzyme will facilitate reduction in adipocytic mass.

This is where GA performs its duties and helps you get skinny, the ultimate result can be attributed to a few proximate causes. Firstly, the vital role of GA and cortisol. By reducing the local availability of cortisol via 11HSD-1 inhibition (28), GA causes a reduction in the concentration of intracellular triglycerides (29), in addition to impeding the differentiation preadipocytes(30).

The merits for topical applications of GA are not limited to the above, but further investigation also showed the ability for GA to positively affect fat metabolism by inactivating fat lipase and increasing mobilization of adipose stores (31).


Here is the full write up,with all scientific referances noted and available via Pubmed.com

http://www.avantresearch.com/products/napalm/research



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Old 05-04-2008, 01:10 PM   #8
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my question concerns the molecular weight of formestane, and if 1 or 2 grams could be added to napalm. if the answer is no, what is a localized carrier that would work. imo formestane would be a great spot reducer to add to a local carrier, particularly one as effective as napalm.
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Old 05-04-2008, 04:47 PM   #9
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Quote:
Originally Posted by thebigt
my question concerns the molecular weight of formestane, and if 1 or 2 grams could be added to napalm. if the answer is no, what is a localized carrier that would work. imo formestane would be a great spot reducer to add to a local carrier, particularly one as effective as napalm.
It's not going to work so well in a hydrophillic carrier. You would want a carrier more akin to Abliterate.
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Old 05-04-2008, 04:52 PM   #10
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Quote:
Originally Posted by thesinner
It's not going to work so well in a hydrophillic carrier. You would want a carrier more akin to Abliterate.
never got to try it before it was dc'd. got any ideas for a local carrier, that would be good for formestane. to bad the napalm wouldn't work.
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Old 05-04-2008, 10:01 PM   #11
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Lipo-U is an ampiphilic carrier.



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Old 05-05-2008, 05:31 AM   #12
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Quote:
Originally Posted by Rodja
Lipo-U is an ampiphilic carrier.
thanks, how many grams of form could i add? ive heard it's almost saturated. also how much trouble will it be to get the form mixed in the lipo? again, thanks. been looking for localized carrier for form.
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Old 05-05-2008, 01:27 PM   #13
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Quote:
Originally Posted by thebigt
thanks, how many grams of form could i add? ive heard it's almost saturated. also how much trouble will it be to get the form mixed in the lipo? again, thanks. been looking for localized carrier for form.
Not too much, maybe 2 grams, but I am not sure how soluble formestane is, so it might be a pain in the ass to mix.



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Old 05-05-2008, 02:06 PM   #14
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Form is a pain in the ass to mix. I would not attempt more than a gram into the already close to saturated Lipo-Ultra.



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Old 05-06-2008, 07:47 AM   #15
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Quote:
Originally Posted by dsade
Form is a pain in the ass to mix. I would not attempt more than a gram into the already close to saturated Lipo-Ultra.
would adding just 1 gram of form even mak