Synephrine

Synephrine is a biogenic amine derived from the Citrus aurantium fruit, which is used for a variety of reasons in Traditional Chinese Medicine. It can be used both to aid in fat loss and as an appetite suppressant and animal models indicate that it may aid in alleviating depression. Synephrine is an adrenergic amine that enhances the metabolic rate, increases fat burning and spares muscle protein. Derived from Citrus aurantium, it is a natural alternative to ephedrine, providing maximum weight-loss results without the side effects of Ephedra.

Synephrine binds with the Beta 3 cell receptors to increase the rate at which fat is released from body stores (lipolysis), along with increasing the metabolic rate. It offers all of the advantages of a stimulant, without the drawbacks. Weight loss clinics throughout the USA are now reporting improved rates of weight loss while using Synephrine without the side effects of ephedrine. Clients have reported up to a 42% reduction in total body fat after using Synephrine.

Ctrus Aurantium is the herbal name for the Chinese Green orange "Zhi Shi". In Chinese folk medicine Zhi Shi was commonly used to treat indigestion and relieve abdominal distension. Recently, the herb has been used in the treatment of shock, heart conditions and cardiac exhaustion. Citrus Aurantium, also known as Bitter Orange or as Seville Orange, was known to the early Greeks, and was probably the first orange grown in Europe (twelfth century). The unripe peel contains appreciable quantities of neohesperidin (14%), and five adrenergic amines (synephrine, N-methyltyramine, hordenine, ocdtopamine, and tyramine). In addition, the extract of Citrus aurantium also contains octopamine. Octopamine appears to play an important role in insect behavior -- the fruit probably contains the compound in order to stop insects from eating it. In humans, octopamine has been called a "false neurotransmitter," which changes brain function, and causes the pituitary to secrete growth hormone.

Synephrine is the main "active" compound found in the fruit of a plant called Citrus aurantium. The fruit is also known as zhi shi (in traditional Chinese medicine), and as green orange, sour orange and bitter orange in other parts of the world. Synephrine is chemically very similar to the ephedrine and pseudo-ephedrine found in many OTC cold/allergy medications and in a number of weight loss and energy supplements which contain Ma Huang. But synephrine differs from ephedrine in that synephrine is considered a semi-selective sympathomimetic (because it targets some tissues such as fat, more than it targets others such as the heart) versus a non-selective sympathomimetic (like ephedra which targets many tissues equally and thus often causes side effects). For example, although some high-dose ephedra-containing supplements have been associated with certain cardiovascular side effects as elevated blood pressure and heart palpitations, researchers at Mercer University in Atlanta have shown that Citrus aurantium extract (because it targets fat tissue rather than heart tissue) has no effect on hemodynamics such as heart rate and blood pressure.

Synephrine is a stimulant, similar to caffeine and ephedrine and it is thought to have similar effects in terms of providing an energy boost, suppressing appetite and increasing metabolic rate leading to the burning or more calories. It is used as a safer alternative to Ma Huang and through its stimulation of specific adrenergic receptors (beta-3, but not beta-1, beta-2 or alpha-1), synephrine is theorized to stimulate fat metabolism without the negative cardiovascular side effects experienced by some people with Ma Huang. Because synephrine is a mild stimulant similar in some ways to caffeine and ephedrine, it is thought to have similar effects in terms of providing an energy boost, suppressing appetite, and increasing metabolic rate and caloric expenditure. In traditional Chinese medicine, zhi shi is used to help stimulate qi (pronounced chee, and defined as the body’s vital energy or life force) – but in order to maximize the metabolic benefits of these extracts, total synephrine intake should probably be kept to a range of 2-10 mg/day. Although synephrine and several other compounds found in zhi shi are structurally similar to ephedrine and are known to act as stimulants (via adrenergic activity), zhi shi does not appear to have the same negative central nervous effects of ma huang (ephedra). Through its stimulation of specific adrenergic receptors (beta-3, but not beta-1, beta-2 or alpha-1), zhi shi is theorized to stimulate fat metabolism without the negative cardiovascular side effects experienced by some people with Ma Huang (which stimulates all beta-adrenergic receptors).

The mechanism of action of synephrine is relatively unique among weight loss aids. Synephrine is an agonist of the alpha(1) adrenoreceptor, which is involved in many physiological processes. This adrenoreceptor plays a variety of roles in adipose tissue, such as modulating intracellular Ca2+ and protein kinase C levels and glycogenolysis and lactate production. Correspondingly, alpha(1) agonists increase lipolysis in a variety of experimental paradigms, including an in vivo increase in lipolysis in human white adipose tissue. This effect is potentiated by beta receptor stimulation, adenosine antagonism, and elevated cAMP levels, so ephedrine, caffeine, and forskolin may all be synergistic with synephrine. The appetite suppression caused by some agents is also known to be due to alpha(1) agonism, so synephrine can also be expected to aid in a fat loss plan in this regard.

Chemical Name: 1-(4-Hydroxyphenyl)-2-(methylamino)ethanol
Molecular Formula: C9H13NO2
Molecular Weight: 176.2
CAS No.: 94-07-5