Great thanks to "Par Deus" of Avant Lab's
for contributing this description.
One of the major contributors to body weight homeostasis in the human
body is the sympathetic nervous system, the principal components of which
are the catecholamines (epinephrine and norepinephrine) and the andrenergic
receptors. There are two types of adrenergic receptors, alpha and beta,
as well as subtypes of each -- and depending on which are activated, lipolysis
(breakdown of fat) can be either stimulated or inhibited.
The most well-known adrenoreceptors to bodybuilders
are the beta receptors. These can be divided into subtypes 1, 2, and 3
-- and it is through these receptors that drugs such as the ephedrine/caffeine
stack and Clenbuterol exert their effects. While Clenbuterol acts directly
on beta 2 receptors, ephedrine exerts its effects indirectly by stimulating
the release of norepinephrine (NE), the body's primary endogenous thermogenic
hormone. Unlike Clenbuterol, NE is not selective in its binding. In addition
to binding to the beta 2 receptor, it also binds to both alpha receptors,
as well as the beta 1 and 3 receptors. It is in regards to its binding to
the alpha 2 receptor that yohimbine comes into play.
Norepinephrine and Yohimbine
Ativation of the alpha 2 receptor inhibits the release
of NE. Thus, by binding to this receptor, NE functions as its own negative
feedback signal. In other words, it shuts off its own release. Obviously,
this is not a good thing for fat loss. This is particularly true at rest
(which, unless you are a marathon runner is 95% of your day) -- this is
because alpha 2 receptors are activated at lower catecholamine levels than
are the beta receptors (1). Thus, thermogenesis is basically always turned
off. It is the differences in regional distribution of alpha 2 and the beta
receptors that is responsible for the gender differences in bodyfat storage
(2). Basically, females have a large number of alpha 2 receptors and few
beta receptors in the gluteofemoral area (hips, thighs, and butt), while
men have the same problem in the midsection. With exercise or the use of
compounds such as the ephedrine/caffeine stack, catecholamine levels can
be increased to a point where the alpha 2 induced inhibition of lipolysis
is partially overcome (1). However, even then, the alpha 2 receptors ARE
still acting to reduce lipolysis. Yohimbine is a selective alpha 2 antagonist
(3) and can thus short circuit this feedback loop, maximizing NE levels,
thus maximizing fat loss, particularly in these problem areas.
Blood Flow
A second, more indirect, mechanism by which Yohimbine
can aid lipolysis via the adrenergic system is by increasing peripheral
blood flow (4, 5). Adipose tissue is known to have rather poor vascularity.
When triglycerides are broken down into free fatty acids and glycerol
during lipolysis, they must also be transported away from the fat cell
or they risk being reincorporated into adipose tissue. Beta receptor activation
causes vasodilation, thus increasing blood flow, however, it does not increase
enough to remove all of the free fatty acids released during lipolysis (6).
Alpha 1 and 2 receptor activation, on the other hand, causes a decrease
in blood flow (2, 7). Thus, antagonism of the alpha 2 receptor with yohimbine
would be expected to increase blood flow, and thus increase the mobilization
and disposal of these FFA's, further aiding fat loss.
Yohimbine vs. yohimbe
Quite a bit of confusion seems to exist about the difference
between Yohimbine and yohimbe. Yohimbine is the principal alkaloid from
the herb P. yohimbe. However, there are 31 other yohimbane
alkaloids that can be present in herbal yohimbe preparations. Some of
these have different and unknown selectivities and potencies (and thus,
effects) at the adrenergic receptors (8, 9) -- in addition, these preparations
vary greatly from brand to brand and even from batch to batch, as no standardization
for extraction exists. In fact, a recent investigation found that most over
the counter preparations have little to no actual yohimbine (10). And,
even in the more potent preparations, most people find a higher degree of
undesirable effects with the herb vs. pure Yohimbine (due to the afore mentioned
31 other yohimbane alkaloids that can be present). With 1Fast400's Yohimbine
Hydrochloride, you are guaranteed 2.5mg of pure, pharmaceutical grade Yohimbine
HCl per capsule, without the added side effects from other alkaloids -
thus, allowing safer, more reliable dosing.
Dosing
Studies have concluded that the ideal dosing for Yohimbine
is .2mg/kg (11) -- this would be 20mg for a 220lb person. Studies using
smaller dosages have produced less favorable results. At this level, little
to no side effects have been reported (Keep in mind, this is with Yohimbine
HCl, not the
yohimbe herb). Another thing to be considered when using yohimbine
is that insulin completely blunts its lipolytic effects, thus it should
ideally be used on a low-carb/ketogenic diet, or at the very least, first
thing in the morning on an empty stomach, followed by moderate aerobic activity
for an extended period.
Amount per 1/4 tsp:
240mg
Packing Information:Each powder is put into a HDPE container, Heat Sealed, and labeled with dosing based off 1/4 tsp. Some items may be hygroscopic and may clump during shipment. This does not effect the efficacy of the product, but just the texture.
Extendend Information:
When making custom topical formulations, we use
Avant Labs Lipo Gel in conjunction with this lipolytic agent to provide superior suspension and absorbtion.
(This substance may be offered in larger bulk. Please call for extended bulk order prices.)
