A Replacement for Ephedrine!
In recent years, an array of different compounds has been launched, each touting their place as THE ephedrine replacement. In fact, even before ephedrine was removed from the marketplace, as misuse and ignorance of ephedrine increased, several manufacturers and marketers scurried and scavenged, looking for a legitimate replacement for the powerful, albeit misunderstood compound.
The recipe for a replacement candidate seemed simple enough, but as history has shown us, finding a naturally-occurring compound that delivered the same, or even close to the same, physiological characteristics was no easy task. Compounding the replacement efforts is the fact that there will probably never again be as much scientific data on a “generic” compound like there was with ephedrine. The heavy burden of profitability is just too strong and those with the means (i.e. pharmaceutical companies) will never fund significant research; but enough with the politics.
First and foremost, ephedrine was known for its fat loss properties. Documented evidence suggests that on average, ephedrine increased weight loss 1.3 lbs. per month more than placebo and combinations of ephedrine or ephedra with caffeine or herbs containing caffeine (EC of the ECA stack) resulted in an average weight loss of 2.2 lbs. per month.
Secondly, the ancillary characteristic of ephedrine-induced fat loss is its ability to preserve muscle mass. This facet of ephedrine makes the net change in body composition so much more dramatic. Losing weight is one thing, but losing weight while keeping the precious metabolically-active muscle, is another, more complicated feat.
And lastly, completing the fat-loss triumvirate are ephedrine’s anorectic properties. So fat loss is triggered, muscle mass is preserved and hunger is kept at bay. No wonder there was such frenzy around this compound — it worked like crazy, it was readily available everywhere.
Not to be downplayed, and certainly not unrelated to its fat-loss properties, but another reason why so many folks wanted to wrap their hands around their favorite bottle of ECA Stack, was because ephedrine, especially riding in tandem with caffeine, was one hell of a stimulant. It does this by triggering a fireworks show of catecholamines, a major group of chemically-related excitatory neurotransmitters that light up your sympathetic nervous system. Ephedrine triggers your body to produce norepinephrine (aka noradrenaline), epinephrine (aka adrenaline), and dopamine.
The primary mechanism of ephedrine, like its chemical cousin amphetamine, is to trigger a release of norepinephrine. This increases the amount of norepineprhine in the synaptic space compared to normal conditions and leads to more adrenergic receptors stimulation (see above). This results in various responses including bronchiole dilation, increased energy expenditure, increased heart rate and blood pressure and a heighted, fight-or-flight state. In addition to the vesicle dump triggered by ephedrine, the molecule itself can also bind directly to adrenergic receptors to mimic the actions of norepinephrine.
As we mentioned above, both the stimulant and fat-loss properties are certainly intertwined and are definitely not exclusive events.
Also, it is important to note that there are 2 types of adrenergic receptors, alpha and beta, each with subtypes, which are targets of the aforementioned catecholamines. Stimulation of alpha (1) and beta (1,2,3) through facilitating the release of norepinephrine and epinephrine are what made ephedrine so special, but as we will see, it was ephedrine’s over stimulation of beta-1 that caused an intervention.
Tripping the switch on the alpha (1) adrenoceptor is responsible for erasing your appetite and might account for the majority of weight loss in subjects using ephedrine. But tripping the switches in the beta set of receptors does some good and some bad. These receptors trigger thermogenesis and also cause the peripheral effects like heart rate increase to happen.
This is by no means an exhaustive explanation of what goes on in ephedrine mediated fat loss, but it gives you framework to use while we look at where we’ve been and where we’re going on this quest to replace ephedrine.
Now there will be those that will argue that the adrenergic pathway is not the best pathway to fat loss, but those arguments are beyond the scope of this piece. What we’re looking for now, is how do we replace ephedrine?
So Now What?
Since ephedrine is gone – or at the very least is available in a limited fashion – several would-be replacements have been pushing and shoving their way into various formulas since ephedrine’s departure. But do they work? Do they provide the same effects that made ephedrine the gold standard?
Or, given the new rules, whether they be from regulatory agencies or even insurance companies refusing to cover ephedrine-containing products, are these new entrants the best we can hope for? Should we be looking to one ingredient, a pair or a triad (or more) to get us where we want to go?
The Other Players.
So if structure leads to function, and it often does in biological systems, then why haven’t we received manna from other catecholamine-like structures?
Synephrine was the first compound in the ephedrine replacement parade. Because it was found in fairly decent amounts in nature in the Bitter Orange fruit, Citrus aurantium, and it exhibited structural similarities, it seemed like the likely candidate to sit in the king’s chair. But despite a fairly researched heritage, synephrine’s reign at the top was short-lived. Why?
Well, despite a trademarked C. aurantium extract having use patents that covered the holy trinity of fat loss — appetite suppression, thermogenesis and muscle sparing — the anecdotal reports were meager at best. At the end of the day, synephrine just didn’t work like we had all hoped. So what about its methylated cousin, methylsynephrine?
Methylsynephrine: An Ephedrine by any Other Name — Methylsynephrine is certainly a darling on the message boards, but what looks extremely promising structurally, especially when you see the other the nomenclature para-hydroxy ephedrine, seems to only deliver those anticongestive properties that its un-methylated cousin provides.
Runny nose? Great. Asthmatic? You’re all set. But unfortunately, unless methylsynephrine is baked into a chemical goulash masking its shortcomings, its 15 minutes of fame (and free parking) are rapidly ending.
PEA — Phenylethylamine (PEA) is an endogenous neuroamine that improves mood very rapidly; again, when produced endogenously. Due to its neuro-modulating actions, PEA plays a pivotal role in the feed/reward mechanisms of dietary behavior and it is this rationale that drove it addition to most of the recent fat-loss items on the market today. But there’s a problem with PEA. The problem stems from its administration and its inability to survive enzymatic deactivation. The absence of the methyl group on the side chain of PEA (versus its presence in ephedrine) makes it easy pickings for enzymatic deactivation by monoamine oxidase, which decomposes these kinds of naked amines.
Geranamine — 1,3 Dimethyl-pentylamine stormed the scene after one of the industry’s most infamous characters put it in one of his fat-loss products. As you can see, it doesn’t fall into the same structural neighborhood (no aromatic ring) as all the other molecules we’ve discussed, but it does carry some stimulant characteristics, albeit far less than ephedrine and is probably a better nasal decongestant that it is a fat burner.
Even though the aforementioned compounds are decent stimulants, to date, the world just isn't happy with them, especially when they are measured against what can only be described as “mythical reputation” of ephedrine.
But that hasn’t stopped us, the consumers, for clamoring for every new hopeful on the diet shelves across the country and the web. Several popular products have taken the above ingredients, plus a few more, to fill the vacuum created by the ephedrine exodus.
A Parade of Mediocrity.
Popular products like the Lipo 6 family of fat burners (and there are a lot of them) were built on the backbone and promise of synephrine and driven by one of the most prolific advertising campaigns in recent years. Hydroxycut and its multiple incarnations, once driven by caffeine and hydroxy citric acid (HCA) is now a veritable clown car of ingredients — so many stuffed into the formula that it is either comical or scary.
But in the land of the blind, the one-eyed man is king, right? Yes. That’s what it looks like. With no ephedrine to keep things simple, formulators and the brands that enslave them, are swerving all over the road, with no depth perception. Some of them make it where they want to go, and we as consumers are happy… or are we?
Can This be Done Better?
Remember our ECA Stack mentioned above? And remember how simple it seemed, at least on paper, to replace ephedrine? All we need to do is find an adrenergic agonist that is not illegal, appears in nature, and oh yeah, since the rules have changed, it cannot carry a laundry list of side effects. AND one final characteristic, it cannot be used by ne’er-do-wells to make illegal drugs. Sheesh.
Now, there is another ingredient that seems to be set to the game-changer. This compound goes by a several, hard-to-remember chemical names, but we’re calling it Halostachine.
Halostachine mimics ephedrine in CNS stimulation, nutrient partitioning and in fat burning. In addition, this is a naturally occurring molecule found in the botanical Halostachys caspica. And while almost identical in structure to ephedrine, Halostachine does not carry the heavy side-effect baggage that gave ephedrine the criminal reputation in the first place. You experience the coveted beta-3 stimulation without the over-the-top stimulation that makes your heart do the 23 Skidoo.
Elegance in Simplicity!
So with a viable candidate for ephedrine now available, we can revert back to the simple and effective recipe of the ECA Stack, obviously without the E. Halostachine coupled with physiologically-significant amounts of the workhouse compounds Caffeine and Salix alba extract standardized for salicin as a natural substitution for Asprin is now the most promising formula built on the heritage that made fat-loss items the darling of our industry.
The Game Changer!
Look, there are a ton of other fat burners out there with most of the recent offerings trying to interrupt the feed/reward mechanism that drives a lot of bad food behaviors. Products like Lipo-6 Black, Redline, Hyperdrive, Meltdown and Hydroxycut are all operating on various angles. Vapor XT™ , the only product to incorporate the new Halostachine Stack is not a formula littered with ill-performing, label-fluffing ingredients.
Vapor XT™ will be the most reliable, predictable and controllable recomp/cutting companion. Because as we know, it’s not really a game when it comes to stripping away bodyfat, it is indeed a war.
Arm yourself for the war now!
Order Vapor-XT now. It's as simple as that.
Thanks for your continued support,