Alpha-2 Adrenoreceptor Downregulation

Understanding the Problems

The class of receptors, once activated, will make the fat cell shrink. The other class of receptors when activated will make the fat cell bigger and prevent it from shrinking. This is the balance between the good and the bad receptors which will determine how fat you are. Furthermore, those good and bad receptors are not equally spread on each fat cells. Some cells contain more good receptors and so are easily shrunk by a diet. But many fat cells contain more bad than good receptors. This is why some fat deposits are very hard to lose. Which means you will never get lean in those areas unless you reduce the number of the bad “Dirty” receptors.

Alpha-2 Receptors: The Enemy

You have heard of them before. Their exact name is alpha-2 receptors for simplification. They are not the first line of defense for our fat cells. The first line of defense among the bad receptors are insulin receptors. But once you go on a low calorie diet, especially Dan Duchaine’s BodyOpus diet, your insulin level will go down. There will not be enough of that hormone to prevent fat cells from shrinking. Once the body realizes its first line of defense is out of order it calls upon the second line of defense: it increases the responsiveness of each alpha-2 receptor. From a dieter’s point of view, this means he will then be unable to lose fat where a high density of alpha-2 receptors can be found.

Alpha-2 Receptor Densities

It is easy to figure out where the alpha-2 receptors are the most dense just by looking at someone. This is exactly where their fat accumulates. You see, alpha-2 receptors not only prevent fat loss but they also promote fat gains. They are like magnets, attracting and retaining fat. Alpha-2 receptors are found in very high densities below the skin (subcutaneously). We can distinguish two main patterns of alpha-2 distributions:

  1. In most women and in some men with a female type body fat distribution, alpha-2 receptors are found in high density mostly on the subcutaneous fat of the butt and of the legs.
  2. In most men and in some women (those neither showing a specific lower body fat accumulation), most of the alpha-2 receptors are located equally all over the subcutaneous fat of the body.

Subcutaneous vs Intramuscular Fat

The subcutaneous fat is the fat located between the skin and the muscles. This is the fat that if carried in excess will make you look fat in a mirror. Intramuscular fat on the other hand is the fat that we find inside the muscles. You can have plenty of intramuscular fat and not look fat. In fact, if one only carries intramuscular fat with virtually no subcutaneous fat, he will look big and lean even though he really is fat.

In reality, most people will carry more subcutaneous fat than intramuscular fat. This is bad enough, but as you go on a diet, things turn ugly. As we said above, the subcutaneous fat contains the most alpha-2 receptors (around twice as much) when compared to intramuscular fat. So when you go on a diet, you will lose intramuscular fat twice as easily as subcutaneous fat. In front of a mirror, this is a catastrophe: by losing intramuscular fat, your muscles will appear smaller. But since little subcutaneous fat will be lost, you will not look much leaner. In fact, you will only see a smaller (but not leaner) version of yourself. All this because of those extra alpha-2 receptors.

To sum it up; people with much of their bodyfat as subcutaneous fat will lost fat but in the wrong place and so will not appear leaner where they want to. Alpha-2 adrenoceptors are the main culprit. Before being able to combat those receptors, we first have to understand which factors increase alpha-2 numbers on our fat cells.

When the Betas Control the Alphas

We have said above that there were two big classes of receptors on fat cells; the good ones and the bad ones. So far we have talked of the bad ones. The good ones are called beta receptors. Like alpha-2 receptors, they are found on the fat cells. When activated, these beta receptors will try to shrink the fat cells. But they will only succeed if the alpha-2 receptors are not found in too high quantity in those cells. You see, alpha-2 receptors have exactly the opposite effects of beta receptors. As both are activated by the same hormones (adrenaline and noradrenaline), if a higher quantity of alpha-2 receptors are found, beta receptor effects will be overwhelmed and no fat loss will occur in those receptors. Beta receptors will only induce fat loss on fat cells with low alpha-2 density. That is the area where it is easy to lose fat while on a diet (mostly intramuscular fat).

As if things were not bad enough, each time beta receptors are activated, two signals are sent to the fat cells:

  1. To either increase the number of alpha-2 receptors or their responsiveness or both.
  2. To either decrease the number of beta receptors or their responsiveness or both.

This means that within a few days you will have a stronger alpha-2 response to the hormones which are supposed to make you leaner (remember adrenaline and noradrenaline) and a weaker beta response. That is bad, really bad. You now understand why will have to get dirty!

Playing Russian Roulette With Low-Calories Diets and Alpha-2 Receptors

A second factor which controls alpha-2 receptors on fat cells is the diet itself. As your calorie intake goes down, so will the level of insulin in your blood. As we said above this will increase the responsiveness of each alpha-2 receptor in the short run. This is bad but not terribly bad as it will also increase both the number and the responsiveness of the good receptors (beta receptors). But after a few days of dieting, most people will get lucky. The number of alpha-2 receptors will decrease a little. Some people will be unlucky though, as either their number of alpha-2 receptors will go up or the responsiveness of each alpha-2 receptor will increase. Even worse, in some people both the number and the responsiveness of the alpha receptors will increase. We all know who they are; those who cannot lose ft no matter what (that is until now). So the impact of dieting on alpha-2 receptors looks more like Russian Roulette than a science. And even on the luckiest, the favorable effects of diets on alpha-2 receptors will be mild.

Exercise and Alpha-2 Receptors

Exercise does not seem to help get rid of alpha-2 receptors. In fact, if exercise has an impact on alpha-2 receptors on fat cells it would tend to be an up-regulation. But most studies show no impact at all. This has a direct consequence especially for women (but this also applies to men). We said that the major reason why women have a hard time losing fat on the butt is because the density of alpha-2 receptors on that body part is too high. Furthermore, we just saw that exercise will not help to down-regulate alpha-2 receptors.


Don’t waste your time doing endless repetition with a light weight on butt blaster or doing high rep lunges. This might burn off a few calories but it will not solve the problem. This is also true for men doing endless repetitions of sit ups for abdominals to fight subcutaneous fat on the stomach. I know this will not prevent you from doing it but at least now you understand why you get nothing out of it!

Originally published in Dan Duchaine’s Dirty Dieting Newsletter

Yohimbex (yohimbine hydrochloride)

Yohimbex (yohimbine hydrochloride)

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