Thermics Information
THERMICS

STIMULANT-FREE ADRENERGIC WEIGHT-LOSS STACK

NO EPHEDRINE, CAFFEINE or ASPIRIN!

Thermics is a stimulant-free diet aid that takes a new approach to adrenergic weight loss. Our patented* formula supports lipolysis (fat oxidation) without the use of ephedrine alkaloids or caffeine, so you are not faced with the uncomfortable jitters and restlessness often associated with stimulant-based thermogenics. At its core are octopamine and yohimbine, a potent beta-3 receptor agonist and alpha-2 antagonist respectively, which trigger two pathways vital to fat loss but devoid of strong central nervous system activity. Bergenin and decaffeinated green tea extract (high in levels of epigallocatechin gallate) are added for their abilities to enhance adrenergic lipolysis without direct CNS stimulation, allowing us to create the first truly effective and comfortable replacement for E/C/A.

Octopamine

Octopamine is a potent naturally occurring selective beta-3 adrenergic receptor agonist1, and has been shown in in-vitro animal studies to exhibit strong lipolytic activity in fat cells2. It is also the first selective beta-3 agonist ever to be isolated and made available as a nutritional supplement, and given the understanding we have of beta-3 receptors and their ability to mediate human fat loss we believe it holds tremendous promise as a powerful, comfortable and safe fat-loss alternative to a non-selective beta agonist like ephedrine.

Beta-3 adrenergic receptors have been isolated in both human white3 4 5and brown6 7adipose tissues, and are now understood to play an important role in lipolysis and thermogenesis in our bodies8 9 10. They are vastly more important here than previously thought by scientists, who had difficulty in the past discerning the contribution of each beta-receptor subtype (beta 1,2 and 3) without having agents selective for each to investigate. Early reports were actually not in favor of beta-3 receptors having much of a role in adult humans, or even being present in fat tissues at all11. During the mid to late 1990's our view of this receptor finally began to change, however, with the publishing of a number of new studies. One such paper concerns an investigation into ephedrine12. Using beta-receptor blocking agents (antagonists), investigators were able to demonstrate that beta-3 agonist activity likely accounted for at least 40% of the thermogenesis induced by this weight loss drug. Its strong action here seems not to be due only to beta-1 and beta-2 activation as we incorrectly believed earlier. Several other papers, as are referenced above, reported the isolation of beta-3 receptors in human fat tissue around the same time, and further demonstrated its role in triggering lipolysis and thermogenesis.

When a synthetic selective beta-3 agonist was finally developed and studied in human trials in 2001, the notion that this type of agent could actually be an effective weight loss option became an unquestionable fact13. During these trails a group of 12 otherwise healthy overweight men noticed a clear increase in lipolysis, as well as total energy expenditure, with the use of a beta-3 agonist exclusively. We are sure the intended action of the drug was solely responsible for these effects because heart-rate and diastolic blood pressure did not increase in any of the subjects (signs that non-selective beta agonistic activity were occurring), nor did the concentrations of the endogenous adrenergic hormones epinephrine and norepinephrine. Leptin, a hormone often relevant to weight loss, also did not change during the study. We are left with proof that beta-3 agonists can be important triggers of lipolysis and thermogenesis in humans, and have opened a new door to weight loss without the uncomfortable jitters and central nervous system stimulation noted with non-selective beta agonists like ephedrine (selective beta-3 agonists do not produce the same strong CNS stimulation14).

Yohimbine

Adrenergic lipolysis in human adipose tissue is regulated in a dual nature by adrenoceptors. Most notably, activation of the beta-1, beta-2 or beta-3 subtype increases the process of lipolysis; while activation of alpha-2 receptors diminishes it (fat cells appear to be the only type of cells in the human body that exhibit such dual regulation by adrenoceptors)15. Yohimbine, sold as a drug in some other countries, is an extremely potent naturally-occurring alpha-2 receptor antagonist (it blocks this receptor instead of activating it)16. Studies with this compound have consistently shown that as a result it is capable of increasing lipolysis in humans after oral dosing, via both alpha-2 receptor antagonism and increases in synaptic norephinephrine release17 18. In effect it serves both beta stimulating and alpha blocking properties, an ideal combination if we want to stimulate fat loss. However, when single doses as high as 21.6mg, or daily cumulative doses as high as 43.2 mg, were taken in these studies the agent was well tolerated, and had no significant impact on blood pressure or heart rate as would be expected of a non-selective beta-agonist like ephedrine.

It is of note that yohimbine seems to work most effectively in the fasted state, and its lipolytic action may be blocked if it is taken with a meal19. For the reason it may be a good idea to take Thermics on an empty stomach.

Epigallocatechin Gallate

Decaffeinated Green tea extract has been added specifically for its high EGCG (epigallocatechin gallate) content, which is thought to be the most pharmacologically active tea catechin in green tea20. Green tea has been around for centuries, and has been used in herbal medicine for about as long. Early on its beneficial properties were noticed, particularly in Asian cultures where is widely consumed and often thought of as a having numerous positive health benefits. In recent years scientists have been investigating the content and actions of Green Tea, and are coming to confirm with solid evidence many of its positive effects including those as an anti-oxidant, cholesterol lowering, antidepressant, capillary-strengthening and lipolysis-enhancing agent. Its inclusion in Thermics is a result of its documented ability to support thermogenesis and lipolysis in human studies21.

Early suggestions were that its caffeine content was solely responsible for this effect; however this belief was dismissed in a study published in 1999 that demonstrated green tea to have an effect that could not be duplicated with an equivalent dose (50mg) of caffeine22. In this investigation green tea increased 24 hour energy expenditure significantly, while the caffeine actually had no noticeable effect at all. It looks now like its high content of tea-catechins, particularly EGCG, which are the source of its positive activity here. Studies with purified EGCG seem to support this notion, showing this catechin to exert a direct effect on thermogenesis by increasing the respiration rate of brown fat cells23. It was further demonstrated to enhance the lipolytic action of ephedrine and caffeine in the same investigation. In-vitro tea catechins were also shown to inhibit the COMT enzyme, which is responsible for degrading the adrenergic hormone norephinephrine24. Since norepinephrine has an important role in human thermogenesis and fat metabolism, this might account for at least some of its positive action here.

In keeping with our goal of a comfortable jitter-free thermogenic we have opted to use an extract high in catechins and EGCG but devoid of caffeine. Our Decaffeinated Green Tea Extract is standardized for 90% catechins and 60% EGCG content.

Bergenin

Bergenin is an isocoumarin found in a number of plant species including Bergenia crassifolia (siberian tea), Mallotus japonicus, Astilbe thunbergii (Ostrich Plume) and Ardisia japonica (Marlberry). It has a long history in Asian and Indian natural medicine, where it can be found in various herbal extract forms purported to exhibit anti-arrhythmia, bronchitis treating, astringent, tonic, anti-obesity and laxative properties. In recent years it has been looked at in western medicine as purified bergenin, with early studies reporting several potential benefits to this agent including anti-hepatotoxic (liver protecting)25 26, antiarrhythmic27 and ulcer fighting28 activities. Like EGCG, bergenin has also been shown to be capable of augmenting the lipolytic action of agents acting on the adrenergic system. Studies have confirmed that while the compound itself does not directly stimulate lipolysis or have measurable adrenergic activity; it markedly enhances lipolysis induced by an adrenergic hormone such as norepinephrine, and even opposes the lipogenic (fat building) actions of insulin29. Its exact mode of action is unknown at this time, but it is believed to involve increased norepinephrine binding to fat cells.

With all 4 agents in place, Thermics represents the most effective and complete approach to adrenergic-mediated weight loss devised without the side effects of ephedrine or other strong stimulants!

How Supplied:

100 capsules per bottle, each capsule containing:

Octopalean (octopamine) 150 mg
Decaffeinated Green Tea Extract 100 mg
(Standardized 90% catechins, 60% EGCG)
Bergenin 100 mg
Yohimbe Extract 37.5 mg
(Standardized 8% yohimbine)

Octopalean is a trademark of Creative Compounds

Directions:

Take 1-2 capsules, 2-3 times per day. Do not exceed 12 weeks of continuous use.

These claims have not been evaluated by the FDA. This product is not intended to diagnose, treat, cure or prevent any disease.

Do not take if you are pregnant or nursing. Consult your doctor before using if you have or at risk for high blood pressure, heart disease, diabetes or are taking any medications.

*U.S. Patent Pending

REFERENCES:

1Selective activation of beta3-adrenoceptors by octopamine: comparative studies in mammalian fat cells. Carpene C, Galitzky J et al. Naunyn Schmiedebergs. Arch Pharmacol 1999 Apr;359(4):310-21

2Effects of octopamine on lipolysis, glucose transport and amine oxidation in mammalian fat cells. Fontana E, Morin N, Prevot D, Carpene C. Comp Biochem Physiol C Toxicol Pharmacol 2000 Jan;125(1):33-44

3Distribution of beta 3-adrenoceptor mRNA in human tissues. Berkowitz DE, Nardone NA, Smiley RM, Price DT, Kreutter DK, Fremeau RT, Schwinn DA. Eur J Pharmacol 1995 Apr 28;289(2):223-8

4Expression of beta3-adrenoceptors with low lipolytic action in human subcutaneous white adipocytes. Tavernier G, Barbe P et al. J Lipid Res 1996 Jan;37(1):87-97

5Clinical pharmacology of beta 3-adrenoceptors. Lipworth BJ Br J Clin Pharmacol 1996 Sep;42(3):291-300

6Brown adipose tissue, beta 3-adrenergic receptors, and obesity. Lowell BB, Flier JS. Annu Rev Med 1997;48:307-16

7Thermogenesis and brown fat: relevance to human obesity. Stock MJ. Infusionstherapie 1989 Dec;16(6):282-4

8Development of beta 3-adrenoceptor agonists for the treatment of obesity and diabetes--an update. Weyer C, Gautier JF, Danforth E Jr. Diabetes Metab 1999 Mar;25(1):11-21

9Clinical pharmacology of beta 3-adrenoceptors. Lipworth BJ. Br J Clin Pharmacol 1996 Sep;42(3):291-300

10Determination of beta 3-adrenoceptor mediated lipolysis in human fat cells. Hoffstedt J, Shimizu M, Sjostedt S, Lonnqvist F. Obes Res 1995 Sep;3(5):447-57

11Adrenergic receptor function in fat cells. Arner P. Am J Clin Nutr 1992;55:228S-36S

12Contribution of beta 3-adrenoceptor activation to ephedrine-induced thermogenesis in humans. Liu YL, Toubro S, Astrup A, Stock MJ. Int J Obes Relat Metab Disord 1995 Sep;19(9):678-85

13Acute effect of L-796568, a novel beta 3-adrenergic receptor agonist, on energy expenditure in obese men. van Baak MA, Hul GB et al. Clin Pharmacol Ther 2002 Apr;71(4):272-9

14Increase in insulin action and fat oxidation after treatment with CL 316,243, a highly selective beta3-adrenoceptor agonist in humans. Weyer C, Tataranni PA, Snitker S, Danforth E Jr, Ravussin E. Diabetes 1998 Oct;47(10):1555-61

15Adrenergic receptor function in fat cells. Arner P. Am J Clin Nutr 1992;55:228S-36S

16Alpha-2 adrenoceptors in lipolysis: A2 antagonists and lipid-mobilizing strategies. Lafontan, Berlan et al. Am J Clin Nutr (1992) 22:219s-27s

17Alpha2-Antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male volunteers. Galitzky, Taouis et al. Eur J Clin Invest (1998) 18, 587-94

18Plasma catecholamine levels and lipid mobilization induced induced by yohimbine in obese and non-obese women. Berlan, Galitzky et al. Int J Obesity (1991), 15, 305-15

19Effects of Yohimbine on Autonomic Measures are Determined by Individual Values for Area Under the Concentration-Time Curve. Grasing, Sturgill et al. J Clin Pharm (1996) 36:814-22

20Physiologically-active plant foods: An overview. Proc Nutr Soc (1996) 55:371-84

21Efficacy of green tea extract rich in catechin polysphenols and caffeine in increasing 24-h energy expenditure and fat oxidation in humans. Dullo A., Duret C et al. Am J Clin Nutr (1999) 70:1040-5

22Green tea and thermogenesis: interactions between catechin-polyphenols, caffeine and sympathetic activity. Dulloo A. Seydoux J et al. Int J Obes (2000) 24:252-58

23Green tea and thermogenesis: interactions between catechin-polyphenols, caffeine and sympathetic activity. Dulloo A. Seydoux J et al. Int J Obes (2000) 24:252-58

24Catechol-o-methyl-transferase: structure-activity relationship for inhibition by flavonoids. Borchardt RT, Huber JA. J Med Chem (1975) 18:120-2

25Antihepatotoxic activity of bergenin, the major constituent of Mallotus japonicus, on carbon tetrachloride-intoxicated hepatocytes. Kim HS, Lim HK, Chung MW, Kim YC. Ethnopharmacol 2000 Jan;69(1):79-83

26Effects of bergenin, the major constituent of Mallotus japonicus against D-galactosamine-induced hepatotoxicity in rats. Lim HK, Kim HS, Choi HS, Choi J, Kim SH, Chang MJ. Pharmacology 2001;63(2):71-5

27Bergenin is the antiarrhythmic principle of Fluggea virosa. Pu HL, Huang X, Zhao JH, Hong A. Planta Med 2002 Apr;68(4):372-4

28Antiulcer activity of naturally occurring pyrano-coumarin and isocoumarins and their effect on prostanoid synthesis using human colonic mucosa. Goel RK, Maiti RN, Manickam M, Ray AB. Indian J Exp Biol 1997 Oct;35(10):1080-3

29Norepinephrine-augmenting lipolytic effectors from Astilbe thunbergii rhizomes. Han LK, Ninomiya H, Taniguchi M, Baba K, Kimura Y, Okuda H. J Nat Prod 1998 Aug;61(8):1006-11

Thermics

*These statements about Thermics have not been evaluated by the Food and Drug Administration. Thermics is not intended to diagnose, treat, cure, or prevent any disease.