Synephrine[edit | edit code]
What is synephrine | |
P-synephrine (aka bitter orange , citrus orange or Citrus Aurantium ) is a protoalkaloid found in the bitter orange extract obtained from the fruit of the citrus orange tree. Can also be found in various citrus fruits such as Seville, mandarin, sweet oranges, clementines, grapefruits. Synephrine is structurally similar to ephedrine, a weight loss supplement banned by the US Food and Drug Administration (FDA) in 2003 due to negative health effects. There are many different isomers of synephrine. The isomers have a similar molecular formula, but differ in physiological effects. P-synephrine found in plant sources, while |
m-synephrine
- a chemical used to burn fat.
While the effectiveness of its isomer p-synephrine
is still in question.[2]. Synephrine has gained immense popularity in the world of sports nutrition as an alternative to ephedrine (a substance that is illegal in most countries). p-synephrine is found in large quantities in citrus auranthium (bitter orange), from which it is extracted for use in sports nutrition. Pharmacologically significant effects have mainly been established for m-synephrine, which has an effect similar to the endogenous hormone adrenaline.
Effects of synephrine[edit | edit code]
- Mobilizes fat depots
- Enhances heat production
- Gives energy
- Speeds up metabolism
- Provides mental focus
- Suppresses appetite
Mechanism of action[edit | edit code]
M-synephrine is similar in structure and mechanism of action to ephedrine, but at the same time, according to the manufacturers, it is devoid of the latter’s side effects, since it does not cause negative effects on the nervous and cardiovascular systems. As a stimulant, synephrine accelerates metabolism, increases the activity of the central nervous system, destroys fats by increasing thermogenesis, and, as a result, helps reduce body fat mass.
The body has alpha and beta adrenaline receptors, these receptors are targets for stress hormones and catecholamines that are released during physical training. Stimulation of these receptors causes a strong sympathetic response: increased heart rate, increased alertness, increased strength, which allows the body to overcome stress. This reaction speeds up metabolism and potential fat oxidation.
M-synephrine is a beta-3 adrenergic receptor agonist, the stimulation of which leads to the mobilization of fat from adipocytes (fat cells). [3]
Alkaloids such as m-synephrine and ephedrine cause a significant physiological response, increasing the metabolic rate and fat oxidation. This is why m-synephrine and other alkaloids are added to weight loss supplements.
What is synephrine? Mechanism of action
From a chemical point of view, synephrine is a protoalkaloid, an organic compound of plant origin, the source of which is tropical fruits. Synephrine has become an excellent replacement for ephedrine. Having a similar mechanism of action, it does not have the disadvantages of a prohibited drug: it does not affect the heart and blood vessels, does not increase the pulse rate and blood pressure numbers.
The mechanism of action of synephrine is realized through the activation of beta-3 adrenergic receptors in adipose tissue, muscles and the nervous system. Like norepinephrine and adrenaline, synephrine increases the activity of the sympathetic nervous system, thereby speeding up the breakdown of triglycerides with the release of fatty acids, which are subsequently oxidized in skeletal muscles.
Role in bodybuilding[edit | edit code]
Synephrine, the supplement most commonly used for weight loss, is primarily a comprehensive fat burning supplement. Additionally, its sympathetic effects can help increase strength, reduce fatigue, and improve overall performance.
Two groups of scientists in 2004 and 2006 reviewed the scientific evidence for the effects of p-synephrine on weight loss. In 2004, scientists concluded that citrus synephrine was ineffective for weight loss and had a lipolytic effect only in high doses[4]. In 2006, researchers stated that there was some evidence of effectiveness and that additional, more rigorous clinical trials were needed[5].
A 2011 study shows that using synephrine in combination with caffeine and green tea extract accelerates fat burning, but the contribution of synephrine to the result is unclear. The same researchers suggested that synephrine has a lipolytic effect and is able to increase metabolic rate by 6.7% without causing any side effects on heart rate or blood pressure [6][7].
There is little information that synephrine affects exercise performance. Currently, there is only one known study that suggests that using synephrine in combination with caffeine may help with moderate-intensity exercise. The study was initially aimed at identifying improvements in exercise endurance[8]. A 2015 study by Nicholas A. Ratamess found an increase in local muscle endurance in strength exercises when using p-synephrine. The effect of p-synephrine was enhanced when combined with caffeine.[9]
Dosages[edit | edit code]
The studies used doses ranging from 13 to 50 mg as a single dose.
Conclusions[edit | edit code]
Studies have found that citrus p-synephrine does not interact with alpha and beta adrenaline receptors
, unlike the m-isomer, therefore does not cause negative effects on the heart and blood pressure. In 2004, the FDA concluded that taking bitter orange extract or p-synephrine at recommended doses did not cause adverse reactions. At the same time, the effectiveness of the p-isomer is extremely doubtful.
Effects of synephrine in fitness and sports
- Lipolytic: stimulates the breakdown and burning of fat.
- Stimulating: increases mental and physical performance.
- Metabolic: speeds up metabolism.
- Thermogenic: enhances heat production.
Synephrine potentiates the body's physiological response to training stimuli. Gentle stimulation of the nervous system leads to an increase in mental focus and motivation, sharpens perception, and creates a positive attitude. Accelerating your metabolism energizes your muscles, giving you the strength to perform extra sets and critical reps beyond muscle failure. It has been proven that taking the drug helps increase strength indicators, in particular, peak power and strength.
Thanks to the lipolytic effect, the destruction of fat is enhanced, and the muscles receive another source of fuel. This fuel is used to cover immediate needs, allows you to save muscle glycogen and pushes back the threshold of fatigue. As a result, an athlete or fitness enthusiast can count not only on rapid fat burning, but also on increasing endurance during cardio and strength training.
Sports nutrition and synephrine[edit | edit code]
Sports supplements contain different doses of synephrine, which range from 3 to 30 mg per dose. In medicine, synephrine is used in much larger doses, reaching 100 mg.[10]
Synephrine is included in the following supplements:
- Animal Cuts from Universal Nutrition
- Lipo-6x from Nutrex
- Tight Xtreme from SAN
- Meltdown by VPX
- Super Nova Caps by Weider
- Anadrox by MHP
- SLIMTABS from Vitamir®
- X-Shred by STL
Side effects[edit | edit code]
Despite the fact that sports nutrition manufacturers present synephrine as a completely safe component, in reality this is not the case. Synephrine has several side effects, especially when combined with other stimulants such as caffeine, tyramine, octopamine and so on. The most common are: increased blood pressure, headache, indigestion, palpitations, tachycardia and others. In general, the side effects are consistent with those of ephedrine, suggesting that synephrine is a weaker analogue of ephedrine. [eleven]
Synephrine - detailed studies
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08.04.2016
Let's face it - the issue of fat burning is extremely relevant and inescapable for a huge number of aspiring and concerned people. Scientists and consumers themselves are constantly searching for optimal solutions to get rid of fat and safely speed up metabolism. Ephedrine and clenbuterol were once widely relied upon until the latter were officially banned in numerous countries (including the United States) due to their extremely high dependence and overall health hazards. Nowadays, active research is underway on a variety of plant extracts, amino compounds, dosages, etc. for a safe but effective effect on the destruction of fat structure. What trends have now prevailed in the world of sports supplements aimed at burning fat? Let's get a look.
If you have used this category of supplements such as fat burners more than once, or have been passionately interested in them, then all you have to do is pay attention to the study of ingredients in order to identify the most frequently used components. Then you will notice that quite a few of them occur frequently and are repeated even in the most “advanced” products. We will now talk about a citrus extract - bitter orange, which can be found in the composition under the name Advantra Z. This is a patented form of bitter orange. This ingredient was put into production a long time ago and has recently become widespread as an active component in fat burners from such well-known companies as Nutrex, BSN, Labrada, Cellucor, Max Muscle, etc. Moreover, bitter orange is even added to the formula of many pre-workout complexes. What does this give? Bitter orange has in its molecular composition protoalkaloids that form the basis of synephrine. And this enzyme has already proven itself in the practice of weight loss and appetite suppression. You can safely treat synephrine as a synonym for bitter orange extract. Is it true that it is safe? Well, this question, first of all, applies to everything that you generally pass through the esophagus. Don’t fall for lazy pseudo-arguments that this and that is slowly killing you. If you think about it, a lot of water also kills you, a lot of coffee kills you, antibiotics kill you, sweets kill you, and fast food is generally poison, not food. But there is such a phrase as “reliable scientific data.” And they, based on repeated studies, claim that bitter orange and synephrine do not have serious adverse effects even at significant dosages. Scientists conducted more than 20 studies on 360 patients and found that bitter orange extract, either alone or in combination with other ingredients (like caffeine, for example), does not produce side effects such as increased heart rate, increased blood pressure, changes in the number of blood cells, urine composition, or changes in electrocardiogram data. It has been found that a cycle of taking pure synephrine for six to twelve weeks in a row has little effect on fat loss, so it is better to mix it with other extracts, which is what many competent sports nutrition manufacturers do. Obviously, synephrine expresses itself most clearly in combination with caffeine. At Baylor University, athletes took a pre-workout matrix of 450 mg of caffeine, 1.2 g of garcinia cambogia, 225 mg of chromium picolinate, and 360 mg of bitter orange extract. Aerobic and anaerobic exercises were carried out, as a result of which the subjects (men and women) with a slight difference recorded a safe but significant increase in metabolism.
Scientists at Montana State University examined sports products containing caffeine, bitter orange extract, and green tea extract for their effects on cardiovascular health in mildly overweight individuals. 14 young women and nine men volunteered to participate in the experiment. They took capsules with 13 mg of synephrine and 176 mg of caffeine. As a result, no negative reactions were identified on the state of systolic and diastolic blood pressure, and heart rate. Thus, consuming food supplements containing moderate amounts of bitter orange extract, caffeine and green tea does not lead to stressful situations in the body and has a positive effect on fat burning. True, with one amendment - continuous use of synephrine is best limited to 12 weeks, since the studies were conducted within this period; In addition, there is no need to abuse dosages, thinking that the more, the more effective. Remember this.
The report from Intertek Cantox (Ontario, Canada) also provides official scientific confirmation that the use of synephrine in combination with caffeine within a given period (12 weeks) does not undermine health at all. Although there is a clarification about the optimal dose: synephrine in its pure form in such cases should not be higher than 60 mg per serving, or 40 mg of synephrine and 320 mg of caffeine. To top it all off, Health Canada, which is known for its monarchical strictness, agrees that bitter orange is widely used in herbal medicine and food, and does not pose any risk to the health of consumers.
Conclusion: in the indicated dosages, synephrine (especially in combination with caffeine) can increase energy expenditure in the body and stimulate fat burning without risk to health.
Links[edit | edit code]
- Stohs SJ, Preuss HG, Shara M. A review of the receptor-binding properties of p-Synephrine as related to its pharmacological effects. Oxidative Medicine and Cellular Longevity. 2011. doi:10.1155/2011/482973.
- https://lenta.ru/news/2016/07/21/fat/
- Carpéné C, Galitzky J, Fontana E, Atgié C, Lafontan M, Berlan M (April 1999). "Selective activation of beta3-adrenoceptors by octopamine: comparative studies in mammalian fat cells." Naunyn Schmiedebergs Arch. Pharmacol. 359(4):310–21.
- Fugh-Berman A, Myers A. Citrus aurantium, an ingredient of dietary supplements marketed for weight loss: Current status of clinical and basic research. Experimental Biology and Medicine. 2004; 229(8): 698-704.
- Haaz S, Fontaine KR, Cuttler G, Limdi N, Perumean-Chaney S, Allison DB. Citrus aurantium and synephrine alkaloids in the treatment of overweight and obesity: An update. Obesity Reviews. 2006; 7(1): 79-88.
- Seifert J, Nelson A, Devonish J, Burke E, Stohs S. Effect of acute administration of an herbal preparation on blood pressure heart rate in humans. International Journal of Medical Sciences. 2011; 8(3): 192-197.
- Stohs SJ, Preuss HG, Keith SC, Keith PL, Miller H, Kaats GR. Effects of p-Synephrine along and in combination with selected bioflavonoids on resting metabolism, blood pressure, heart rate and self-reported mood changes. International Journal of Medical Sciences. 2011; 8(4): 295-301.
- Haller CA. Human pharmacology of a performance-enhancing dietary supplement under resting and exercise conditions. British Journal of Clinical Pharmacology. 2008; 65(6): 833-840.
- "The effects of supplementation with P-Synephrine alone and in combination with caffeine on resistance exercise performance." Nicholas A. RatamessEmail author, Jill A. Bush, Jie Kang, William J. Kraemer, Sidney J. Stohs, Vincenzo G. Nocera, Megan D. Leise, Keith B. Diamond and Avery D. Faigenbaum. Journal of the International Society of Sports Nutrition. 2015 12:35 DOI: 10.1186/s12970-015-0096-5© Ratamess et al. 2015 Received: 10 April 2015 Accepted: 2 September 2015 Published: 17 September 2015
- R. Baselt, Disposition of Toxic Drugs and Chemicals in Man, 8th edition, Biomedical Publications, Foster City, CA, 2008, pp. 1471-1472.
- Jordan S, Murty M, Pilon K (October 2004). "Products containing bitter orange or synephrine: suspected cardiovascular adverse reactions."