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Synephrine and Methyl Synephrine: Lipolytic Potential

What is Synephrine?

Citrus aurantium (also known as Bitter Orange, Sour Orange, and Seville Orange) is a relatively small citrus tree about 5 meters tall with scented white flowers (Fugh-Berman and Myers, 2004). As the name implies, the fruit is quite bitter and for this reason, it is not commonly used for culinary purposes. However, the dried, entire unripe fruit of Citrus aurantium has been used as an Asian herbal medicine primarily to treat digestive problems. More specific to this article, the greatest interest recently has been in the active alkaloids of the Citrus aurantium, synephrine (oxedrine) and octopamine (Nelson et al., 2007), which are structurally similar to epinephrine and norepinephrine, respectively. Both synephrine and octopamine are considered trace endogenous bioamines, with circulating levels noted in the plasma of healthy men and women (D'Andrea et al., 2003). Synephrine has alpha-adrenergic effects and also activates beta-3 receptors (but not beta-1 or beta-2 receptors). These effects highlight the potential mechanism of action of this agent related to thermogenesis and lipolysis.

Compounds contained within the Citrus aurantium, such as synephrine, have adrenergic effects that may result in lipolysis and appetite suppression (Fugh-Berman and Myers, 2004).

Synephrine, Thermogenesis and Fat/Weight Loss

As stated above, synephrine is a chief ingredient in many popular fat/weight loss formulas on the market today. Claims for this ingredient include "increased fat burning", "increased energy", "increased metabolism and thermogenesis", and "increased fat/weight loss". As with many nutritional supplements, the claims are largely unsupported by scientific investigation, in particular at the recommended dosage. Some review articles related to the use of Citrus aurantium (or synephrine) as a weight loss aid indicate that little to no evidence exists for such an effect in human subjects (Bent et al., 2004; Fugh-Berman and Myers, 2004; Preuss et al., 2002), while one recent review suggests that "some evidence is promising" (Haaz et al., 2006).

The use of Citrus aurantium or synephrine as a weight loss agent may be based on a study reporting that both synephrine and octopamine will bind to beta 3-receptors, thereby promoting lipolysis (Carpene et al., 1999). Interestingly, octopamine was found to be superior to synephrine in stimulating the beta 3-receptors, as significance was only noted for the synephrine when given at very high dosages (Carpene et al., 1999). This may be the reason that octopamine has been shown to yield a decrease in body weight when administered to rodents (Bour et al., 2003). However, it should be noted that while beta-3 receptor agonists do have lipolytic effects in fat cells of animals, they appear far less active in human fat cells. That is, Larsen et al. (2002) reported no difference in 24 hour energy expenditure, respiratory quotient, or body composition measures in obese men following 28 days of treatment with a selective beta-3 receptor agonist, when compared to placebo.

There have only been a handful of controlled studies focused on either Citrus aurantium or synephrine, with the inclusion of fat/weight loss as an outcome variable (Armstrong et al., 2001; Colker et al., 1999; Kalman et al., 2000). In each of these studies, the amount of weight lost was slightly greater for those using the supplement compared to those using the placebo. However, in all of these studies the supplement consisted of a combination of ingredients (e.g., Citrus aurantium, caffeine, Ginko biloba, St. John's Wort, etc.). Therefore, it is impossible to determine the independent contribution of Citrus aurantium or synephrine on weight loss in these studies. Clearly, more research involving human subjects is needed to shed light on the potential role of synephrine as a fat/weight loss aid.

Methyl Synephrine, Thermogenesis and Fat/Weight Loss

Considering the above reports related to the minimal efficacy of ordinary synephrine to yield significant effects on thermogenesis and body fat/weight loss, a novel form of synephrine has recently been developed called methyl synephrine. Methylation is a common term used in chemistry and biochemistry to denote the attachment or substitution of a methyl group onto various molecules. In doing so, the scientists who have engineered this compound suggest that the therrmogenic effects of synephrine are greatly amplified, yielding a profound effect on fat/weight loss. While anecdotal "in the gym" accounts of subjects using methyl synephrine have been noted as highly favorable, controlled testing of this novel methylated version is necessary before firm conclusions can be drawn related to its ability to function as a potent lipolytic agent.

Hemodynamic Effects of Synephrine: Safety Issues

One concern many individuals have with synephrine is the possible stimulatory effect on the cardiovascular system, in particular heart rate and blood pressure. The hemodynamic changes following a single dose intake of synephrine containing dietary supplements has been investigated, with minimal increase noted in either heart rate or blood pressure (Bui et al., 2006; Colker et al. 1999; Haller et al., 2005; Penzak et al., 2001). For example, Penzak and colleagues (2001) had subjects consume 8 oz of Seville Orange Juice and water, on two different occasions, and noted minimal difference in heart rate or blood pressure between the two trials. Other studies have noted "statistically significant" differences in heart rate or blood pressure when subjects ingest dietary supplements containing Citrus aurantium (Bui et al., 2006) or synephrine (Haller et al., 2005). However, the increase has been noted as small (e.g., 7-10mmHg in blood pressure and 4-11 beats per minute in heart rate). Therefore, it does not appear that otherwise healthy individuals would experience any adverse outcome as a result of normal, suggested dosing.

Practical Applications of Synephrine

In conclusion, the evidence for the use of ordinary synephrine as a fat/weight loss aid is scant at best. While a few studies have noted small improvements in weight loss when using dietary supplements containing synephrine, the absolute difference between synephrine and placebo groups has been minimal. The novel form of this alkaloid, methyl synephrine, has been touted as a much more potent lipolytic agent. Anecdotal reports indicate this as such; however, clinical trials are needed to confirm these observations. Finally, data indicate only a mild increase in both heart rate and blood pressure with use of synephrine containing dietary supplements. Hence, this alkaloid may be considered safe for supplementation purposes when used as recommended.

Beta-Phenylethylamine as a Dietary Supplement

What is Beta-phenylethylamine?

Beta-phenylethylamine (PEA) is a trace amine found within mammalian brain tissue, in particular within the limbic region (Patterson et al., 1990). Beta-phenylethylamine can be synthesized in the body by the enzymatic decarboxylation of the amino acid phenylalanine. Beta-phenylethylamine and its derivatives are also found in high concentrations within plants (Smith, 1977). Thus, individuals may consume PEA regularly as a component of the diet, as it is found in both chocolate and the oil of bitter almonds. It can also be exogenously taken as a pharmaceutical agent or as a dietary supplement. Regardless of delivery, the effects of PEA (as discussed below) appear to be short lived, in that this substance is rapidly metabolized by type B monoamine oxidase (Bakhle and Youdim, 1976; Cooper and Dourish, 1984).

What are the physiological effects of Beta-phenylethylamine?

Since the discovery of PEA in the 1960s, it has been investigated extensively within neurochemical, neuropharmacological, and neurophysiological contexts. Beta-phenylethylamine has been reported to act on presynaptic dopaminergic nerve terminals to stimulate the release of dopamine (Bailey et al., 1987; Nakamura et al., 1998; Raiteri et al., 1977). Because dopamine is commonly associated with the pleasure system of the brain and considered a "feel good" hormone/ neurotransmitter, PEA has been routinely associated with the feeling of euphoria. Beta-phenylethylamine is also noted to exert similar effects as those of exogenous amphetamines, and is therefore referred to as an "endogenous amphetamine" (Popplewell et al., 1986). The specific outcomes related to these effects are discussed below.

Mood

The association between PEA and improved mood is likely the most well investigated aspect of research associated with this substance. The stimulating effects of PEA are likely related to its role in activating the release of dopamine.

In terms of consumption of PEA as a dietary supplement or nutrient found in food, the increase in dopamine may result in an increase in feelings of euphoria. It may also serve to depress food cravings and appetite (as discussed below). In particular, it has been suggested that the psychoactive effects and feelings of euphoria associated with chocolate consumption are due to PEA. However, it should be understood that PEA likely needs to be consumed regularly and/ or in large quantities in order to see long lasting effects, as it is rapidly degraded by type B monoamine oxidase (Bakhle and Youdim, 1976; Cooper and Dourish, 1984), as mentioned above. Use of type B monoamine oxidase inhibitors can dramatically increase the PEA levels, which has been suggested to potentiate dopamine and catecholamine function in the central nervous system (Yu, 1994).

Activity

Behavioral studies have demonstrated that PEA induces a significant increase in locomotor activity (Cooper and Dourish, 1984; Dourish et al., 1983; Popplewell et al., 1986). This may be due to the amphetamine-like effect of PEA. Such findings may have implications related to increased physical activity, possibly mediating enhanced health and weight loss. That is, if supplemental PEA leads to increased physical activity, the increase in caloric expenditure may be associated with favorable changes in body weight.

Appetite

One early study has demonstrated that acute and chronic administration of PEA (once weekly for four weeks) causes a significant reduction in 24 hour food intake, and causes a dose dependent reduction in body weight gain in rats (Dourish and Boulton, 1981). Interestingly, no tolerance to PEA administration was noted (i.e., the effects did not decrease over time). Although these effects have yet to be confirmed in human subjects, it is possible that similar effects may be observed. If so, administration of PEA may prove as an adjunct treatment during periods of calorie restrictive dieting.

Energy Metabolism

Beta-phenylethylamine appears to regulate catecholamine (epinephrine and norepinephrine; AKA, adrenaline and noradrenaline) concentrations, as its presence has been shown to stimulate blood catecholamine levels and inhibit their reuptake (Patterson et al., 1990). Based on these findings, it is possible that PEA may serve a useful role in lipolysis; that is, the breakdown of stored body fat. This is because the catecholamine hormones act on hormone sensitive lipase, the rate limiting enzyme for fatty acid mobilization from storage sites. They do this through a complex interplay between hormones, receptors, and "second messengers". Both epinephrine and norepinephrine interact with beta-adrenergic receptors located on adipose tissue to ultimately lead to fatty acid mobilization into circulation to be used as a fuel source (i.e., to be "burned"). Therefore, it is possible that an increase in the concentration of PEA can exert a stimulating effect on energy metabolism, as well as on the other aforementioned components affected by catecholamine stimulation (e.g., enhanced mood, excitement, etc.). For this reason, PEA may have a use as a "fat burning" agent. Well controlled studies are needed to investigate this hypothesis.

n-methyl-Beta-phenylethylamine and R-Beta-methyl-phenylethylamine

Novel forms of PEA such as n-methyl-Beta-phenylethylamine and R-?-methyl- phenylethylamine have been used recently in dietary supplement preparations. These forms have been suggested to be more resistance to degradation via type B monoamine oxidase; hence, impart a longer lasting and greater effect of PEA. Moreover, they have been suggested to have a greater ability to cross the blood brain barrier, possibly leading to enhanced feelings of euphoria. Although some early study pertaining to these forms has been conducted (Camp et al., 1970), as with the other areas of investigation, additional study is needed to confirm the above theories.

Summary

Beta-phenylethylamine is a well studied substance that has documented effects on both dopamine release and maintenance of catecholamines. This may translate into enhanced feelings of euphoria, mood, and energy. Moreover, the increase in catecholamine levels may stimulate an increase in lipolysis (fat breakdown), which may prove helpful during periods of calorie restrictive dieting. Novel forms of PEA are currently being used in dietary supplement preparations. While these forms appear interesting and may prove more effective than traditional PEA, further research is necessary to confirm the proposed benefits.

Meltdown® by VPX is one of the most profound scientific fat loss innovation of the decade. Meltdown has a star studded ingredient profile of newly invented exclusive fat loss compounds designed to burn fat faster and longer by kicking up a thermogenic storm! And that's just the tip of a very large iceberg of fat burning science. Meltdown will radically increase energy levels, take mental acuity and alertness into the stratosphere and induce an intense mood-altering euphoric effect that is going to re-write fat loss biochemistry.

The Yohimbine Synergistic Fat Loss Trifecta

Yohimbine is an alpha-2-antagonist which simply means it exerts its fat loss effect by blocking the alpha-2 receptors. Blocking action of the alpha-2 receptors is critical for fat loss because it increases blood flow in adipose tissue and as a result ramps up internal fat metabolism causing previously stored body fat to be released into the blood stream and burned as energy. This process is known as Lipolysis. Yohimbine also works by increasing Norepinephrine (NE) - one of the body's principal lipolytic (fat burning) hormones. The challenge is that when NE is released it stimulates both the alpha and beta receptors. While stimulating the beta receptors causes the desired effect of fat liberation, NE simultaneously also stimulates the alpha-2 receptors which can have the undesired effect of interfering with the process of body fat being burned as energy. Yohimbine is a really cool substance because it exerts a kind of self-protective mechanism by blocking the alpha-2 receptors and guarding one of the body's key fat burning hormones called Norepinephrine. Simply stated, it is almost like Yohimbine has a mind of its own that says I'm going to increase NE to destroy body fat and nothing is going to get in my way.

Because of the sheer fat burning potency of Yohimbine, we analyzed this chemical very closely and now introduce two new forms (along with Yohimbine HCl) of Yohimbine in Meltdown. Consequently, Meltdown contains three specialized forms of the potent fat loss agent, Yohimbine. Along with pure Yohimbine HCl, Meltdown now contains 11-Hydroxy Yohimbine which has unusually long half-life and, therefore, exerts a prolonged research-proven fat burning effect for up to eight hours while increasing norepinephrine levels by up to 56%! This is important because Norepinephrine (NE) is one of the body's principal lipolytic (fat burning) hormones. Further, Meltdown also contains the rare alpha-Yohimbine compound. The scientific marvel is that Yohimbine HCl, 11-Hydroxy Yohimbine and alpha-Yohimbine work synergistically to increases lipolysis. These compounds work particularly well in the stubborn areas of the butt, thighs and abdomen because of the Yohimbine receptor cites concentrated in those areas.

Directions For VPX Meltdown: As a dietary supplement, the maximum recommended serving is three Meltdown capsules. However, begin use with one to two capsules daily to assess tolerance. Never exceed more than three total capsules daily or in a single dose.