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As many of you may already know, alpha-2-antagonists are simply compounds that antagonize the alpha-2-adrenoreceptor. The most popular ones are yohimbine, rauwolscine, and a variety of yohimbe alkaloids.
These 3 categories of alpha-2-antagonist each possess a unique goal-specific attribute, but before we delve into specifics, let's look at how effective these compounds are for fat loss.
The relevant research on this topic shows that yohimbine is extremely effective for fat loss.
Yohimbine: the effects on body compos... [Res Sports Med. 2006 Oct-Dec] - PubMed - NCBI
The researchers didn't just use anyone. They used lean athletes. How lean? Both groups started at roughly 9% bodyfat. To put that in perspective:
So these guys are shredded. And they're active, so they probably have a good deal of LBM. After 21 days of yohimbine supplementation, placebo remained unchanged but the yohimbine group lost about 2% bodyfat, taking them all the way to 7% BF. No significant changes in muscle mass or performance were noted.
So:
3 weeks of Yohimbine supplementation caused a 2% reduction in bodyfat from an already shredded baseline of 9% BF, all the while preserving muscle mass and strength/endurance.
To put this in perspective, again refer to the bodyfat chart. These athletes went from the far right image to the middle image in 3 weeks, without major changes to diet or exercise regimens. That's extremely impressive.
So which form of yohimbine is best? That'll depend on your goals.
Yohimbine possess extreme affinity for the alpha-2-adrenoreceptor, but due to receptor homology with various 5-HT receptors, yohimbine HCl is highly anxiogenic and is clinically used to model panic disorder. The effective dose is 0.2mg/kg in isolation. If you combine any of these alpha 2 antagonists with caffeine or beta-agonists (aka synergists), the necessary dose decreases quite a bit.
Rauwolscine lacks significant activity at the 5HT receptors, but it has its own issues. It's less potent than yohimbine, requiring a markedly higher dose to elicit the same effects. Furthermore, it's partially adrenolytic, as it is less selective than yohimbine on the adrenergic system, partially antagonizing alpha-1- adrenoreceptors.
And then we have the various yohimbe alkaloids like 11-OH yohimbine, that are alpha-2-antagonists (not to be confused with a broad-spectrum extract of alkaloids). These compounds act similarly to yohimbine for fat loss but seem to promote a feel-good energy as well. They also have significantly longer half-lives than either yohimbine or rauwolscine, making them a great choice earlier in the day.
So which one works best? It's goal-specific. The most effective for fat loss will be yohimbine or yohimbe alkaloids. The most effective for someone prone to anxiety will be rauwolscine or yohimbe alkaloids (if you have anxiety disorder, you should not be using any of these).
What works best with alpha-2-antagonists? Well here's a brief physiology lesson. The alpha-2 receptor is an autoreceptor, meaning it is located NOT on the postsynaptic neuron chiefly, but on the pre-synaptic neuron. It acts to PREVENT further release of fat burning catecholamines: this is why we want to antagonize (inhibit) it. It's thought that stubborn fat is particularly rich in these alpha-2-receptors, hence why fat loss is always inhibited in these regions. For those seeking to lose stubborn fat, alpha-2-antagonists are a great option.
Alpha-2 antagonists synergize with anything that potentiates catecholamine release. This means caffeine, exercise, forskolin, and beta-agonists all work exceptionally well with alpha-2 antagonists. Furthermore, because alpha-2 antagonism can increase insulin release, these compounds are best taken fasted. A fasted state promotes the counter-regulatory cascade anyway (increased NE/E), so it's the perfect time to dose these, along with preworkout dosing.
So, in summary:
1. Yohimbine or Yohimbe alkaloids are the preferred choice for fat loss; rauwolscine or yohimbe alkaloids may be preferred if one is prone to anxiety.
2. The recommended dose for yohimbine is 0.2mg/kg BW in isolation. If you take it with synergists, the dose needed is less. Rauwolscine needs a higher dose.
3. These compounds have been found to be extremely effective for fat loss, even if you're already very lean and borderline-contest ready. There is also a considerable body of data showing they help with erections. If there's one supplement to consume orally for stubborn fat loss, it's an alpha 2 antagonist.
4. These compounds synergize with caffeine, exercise, forskolin, or beta-agonists. They should be dosed in a fasted state or prior to exercise for maximum results.
5. Recommended products:
a. PES Alphamine
B. iForce Dexaprine XR
c. ECY (use extreme caution)
d. PES Alpha-T2
e. OxyElite Pro with Purple Top
f. PES Enhanced
g. Muscletech Hydroxystim
h. Athletix Acute FX
*Yohimbine should be avoided in concert with Tyrosine or in those diagnosed with anxiety disorder.
These 3 categories of alpha-2-antagonist each possess a unique goal-specific attribute, but before we delve into specifics, let's look at how effective these compounds are for fat loss.
The relevant research on this topic shows that yohimbine is extremely effective for fat loss.
Yohimbine: the effects on body compos... [Res Sports Med. 2006 Oct-Dec] - PubMed - NCBI
The researchers didn't just use anyone. They used lean athletes. How lean? Both groups started at roughly 9% bodyfat. To put that in perspective:
So these guys are shredded. And they're active, so they probably have a good deal of LBM. After 21 days of yohimbine supplementation, placebo remained unchanged but the yohimbine group lost about 2% bodyfat, taking them all the way to 7% BF. No significant changes in muscle mass or performance were noted.
So:
3 weeks of Yohimbine supplementation caused a 2% reduction in bodyfat from an already shredded baseline of 9% BF, all the while preserving muscle mass and strength/endurance.
To put this in perspective, again refer to the bodyfat chart. These athletes went from the far right image to the middle image in 3 weeks, without major changes to diet or exercise regimens. That's extremely impressive.
So which form of yohimbine is best? That'll depend on your goals.
Yohimbine possess extreme affinity for the alpha-2-adrenoreceptor, but due to receptor homology with various 5-HT receptors, yohimbine HCl is highly anxiogenic and is clinically used to model panic disorder. The effective dose is 0.2mg/kg in isolation. If you combine any of these alpha 2 antagonists with caffeine or beta-agonists (aka synergists), the necessary dose decreases quite a bit.
Rauwolscine lacks significant activity at the 5HT receptors, but it has its own issues. It's less potent than yohimbine, requiring a markedly higher dose to elicit the same effects. Furthermore, it's partially adrenolytic, as it is less selective than yohimbine on the adrenergic system, partially antagonizing alpha-1- adrenoreceptors.
And then we have the various yohimbe alkaloids like 11-OH yohimbine, that are alpha-2-antagonists (not to be confused with a broad-spectrum extract of alkaloids). These compounds act similarly to yohimbine for fat loss but seem to promote a feel-good energy as well. They also have significantly longer half-lives than either yohimbine or rauwolscine, making them a great choice earlier in the day.
So which one works best? It's goal-specific. The most effective for fat loss will be yohimbine or yohimbe alkaloids. The most effective for someone prone to anxiety will be rauwolscine or yohimbe alkaloids (if you have anxiety disorder, you should not be using any of these).
What works best with alpha-2-antagonists? Well here's a brief physiology lesson. The alpha-2 receptor is an autoreceptor, meaning it is located NOT on the postsynaptic neuron chiefly, but on the pre-synaptic neuron. It acts to PREVENT further release of fat burning catecholamines: this is why we want to antagonize (inhibit) it. It's thought that stubborn fat is particularly rich in these alpha-2-receptors, hence why fat loss is always inhibited in these regions. For those seeking to lose stubborn fat, alpha-2-antagonists are a great option.
Alpha-2 antagonists synergize with anything that potentiates catecholamine release. This means caffeine, exercise, forskolin, and beta-agonists all work exceptionally well with alpha-2 antagonists. Furthermore, because alpha-2 antagonism can increase insulin release, these compounds are best taken fasted. A fasted state promotes the counter-regulatory cascade anyway (increased NE/E), so it's the perfect time to dose these, along with preworkout dosing.
So, in summary:
1. Yohimbine or Yohimbe alkaloids are the preferred choice for fat loss; rauwolscine or yohimbe alkaloids may be preferred if one is prone to anxiety.
2. The recommended dose for yohimbine is 0.2mg/kg BW in isolation. If you take it with synergists, the dose needed is less. Rauwolscine needs a higher dose.
3. These compounds have been found to be extremely effective for fat loss, even if you're already very lean and borderline-contest ready. There is also a considerable body of data showing they help with erections. If there's one supplement to consume orally for stubborn fat loss, it's an alpha 2 antagonist.
4. These compounds synergize with caffeine, exercise, forskolin, or beta-agonists. They should be dosed in a fasted state or prior to exercise for maximum results.
5. Recommended products:
a. PES Alphamine
B. iForce Dexaprine XR
c. ECY (use extreme caution)
d. PES Alpha-T2
e. OxyElite Pro with Purple Top
f. PES Enhanced
g. Muscletech Hydroxystim
h. Athletix Acute FX
*Yohimbine should be avoided in concert with Tyrosine or in those diagnosed with anxiety disorder.
