The Permissive Substance
Angiotensin II is a polypeptide which is required for the expression of some (but not all) alpha-2 receptors. This means that without angiotensin II, alpha-2 receptors cannot be developed in some cells. As a result, if we somehow get rid of angiotensin II which is naturally produced by the body, the normal renewal of the alpha-2receptors will not happen. You have to understand that there is a constant renewal of the receptors in any cell. By blocking the formation of a specific receptor type in a cell (for example alpha-2 receptors), after a while there will not be any alpha-2 receptors in this cell. The old receptors will “die” and we will have prevented the new generation of receptors from replacing the old ones.
Viola. No more alpha-2 receptors. The big issue is whether this action of angiotensin II takes place in fat cells. Angiotensin II only acts on alpha-2 receptors which respond to two conditions:
- It seems to have the most effect on alpha-2 receptors of the ‘a’ subtype. This is good as it is specifically these receptors which are found on the fat cells. So, the first condition is filled.
- Angiotension II only acts on cells which are rich in both alpha 2 receptors and angiotensin II receptors. That is where we get lucky. We already know that fat cells are very rich in alpha-2 receptors. Scientists also have known for some time that fat cells are very rich angiotensin II receptors.
The key point to remember here is that on fat cells, angiotensin II is needed for alpha-2 receptors to be normally renewed. If we somehow prevent the formation of angiotensin II we will cause major troubles in the renewal of alpha-2 receptors exactly where we want it: on fat cells.
So all you have to do is to impair the production of angiotensin II and allow time to do the rest of the work for you. Within a few weeks the number of alpha-2 receptors will fall. Easy and effective.
Let Me Introduce The Hero of The Day: Captopril
I will not waste time on explaining how Captopril works. The trade name for this molecule can be Capoten, by Bristol-Meyers. Technically, it is a converting enzyme inhibitor. Let’s just say that it is very effective at preventing the formation of angiotensin II. Captopril has no direct effect on alpha-2 receptors. It is only because it prevents the formation of angiotensin II that it will (indirectly) reduce the number of alpha-2 receptors.
How to Use Captopril
Captopril is a drug meant to combat hypertension. If you already suffer from hypotension, you will have some trouble with it. A first key rule is to start slowly 25 mg (half of a pill) daily is a good start. Once you get used to it, you can increase the doses from one to two 50 mg per day. The second side effect you will see with Captopril is you feel like you want to sleep after you swallow a pill. So, it is best to take it before bedtime and not first thing in the morning. Another side effect you going to see quickly is the loss of water. This is because Captopril prevents the formation of a hormone (aldosterone) which promotes water retention. So, by reducing the secretion of aldosterone, Captopril will force you to urinate more often. Don’t worry though, the diuretic effect of Captopril is only mild.
A more long term side effect of Captopril which is well documented by medical studies is weight loss. Well, here we are. Of course, this weight loss could be due to muscle loss- but this is not the case. In fact, Captopril, if anything, has an anabolic effect on the muscles. This was the reason we started using it. If you think we just made a brilliant discovery, let me tell you it all started by mistake.
The True Captopril Story
I first spotted Captopril for its potentially anabolic properties. A woman with an eating disorder asked me to recommend a drug which would give her muscles but without any virilization. I knew her well as I already helped her with her diet. I figured it was the right occasion to test Captopril I did not change her diet which is supposed to be a bit below maintenance as she will have periodic high calorie intake due to her eating disorder. For some reason, I was unable to see her for two to two and a half months. When I saw her again, she told me she was till taking Captopril as her only drug. She did gain a little bit of muscle but not much. But what struck me the most is the fact she had lost fat in areas where she had been unable to significantly lose fat before. She told me she did not change her diet nor did she have less binge eating phases.
At first, I was not that happy as I was expecting the anabolic effect to be stronger. So I went back to the medical library to figure out the mechanisms by which Captopril allowed her to lose fat where so many drugs and diets failed. That is how I found the relation between Captropril and alpha-2 receptors.
It did not take long before I had the occasion to try Captopril again. This time was on a high level bodybuilder competitor. He was able to get lean everywhere but on his legs. This was due to genetics, as his mother had exactly the same fat pattern as he did. He tried many drugs without success, including strong androgens like Permastril. It did help a bit but it was not enough to bring him up from his usual 4th-5th place finishes up to first place. He was a perfect guinea pig as he had several months before his competition. Of course, he was using drugs but he kept using the same ones at the same dosages. To make long story short, for the first time in his life he was able to see his leg definition the day of the competition.
These two examples illustrate how effective Captopril is at helping to get rid of those alpha-2 receptors in real life and not just in theory.
Limitations of Captopril
- Captopril is not an instantaneous cosmetically gratifying drug. Remember, the alpha-2 down regulation will take at least two months before becoming significant.
- You have to follow a lower than maintenance diet to see good results in terms of fat loss. We said that alpha-2 receptors prevent normal fat loss. It does not mean that you will automatically get lean just because you will have reduced the number of alpha-2 receptors. It only means that diet-induced fat loss will be easier (does not mean easy). It will have a permissive effect on fat loss by allowing you to lose fat where it was not possible before.
- The last limitation is that there is still a line of defense for the fat cells. We said that a low calorie diet reduces insulin and its anti-lipolytic effects. By doing that, it triggers the second big line of defense for the fat cells: the alpha-2 receptors. By partially removing the alpha-2 line of defense, we trigger a new one constituted by antilipolytic receptors called peptide YY located on fat cells too. It means that reducing alpha-2 receptor level will allow you to lose more fat than it would have been naturally possible, but it does not mean you will be able to get rid of all your fat.
But, Captopril will permit you to take a big step forward in the right direction.
Some Proposed Stacks To Get The Most Out of Captopril
Non-androgenic Advanced Stack:
- Captopril 50mg a day
- Yohimbine 10 mg a day
Non-androgenic advanced stack:
- Captopril 50-100 mg a day
- Yohimbine 10-20 mg a day
- Clenbuterol (3 to 6, 20 mcg a day)
- Ephedrine + caffeine can be substituted for clenbuterol
- A thyroid cream + an aminophylline cream applied on the area you want to get rid of.
If you do not have access to a thyroid cream, you can make one. Get 1/2 of cytomel. Crunch it and mix it with DMSO. Apply the aminophylline cream first and then the home made thyroid cream.
To the above stack add an aromatase inhibitor (one and a half cytadren taken in 3 divided dosages throughout the day is a cost effective formula) + strong androgen such as Masteron. For muscle mass, keep your favorite anabolic stack.
In any case, take the Clenbuterol and the yohimbine before working out on an empty stomach.
(Editor notes): Capoten is the most potent of the ACE inhibitors. Unfortunately, it has the most undesirable side effects. There are newer, more benign ACE inhibitors. However, the Alpha-2 down-regulation research has been done only on Capoten. We do not know if the newer drugs will have the same positive effect. For example, because of my kidney disease, Capoten would be a terrible choice for me, so I use Zestril instead. It seems to be reducing my lower body fat, ut it would be interesting to see if there is any better improvement with Capoten. DD
Originally published in Dan Duchaine’s Dirty Dieting Newsletter