Exercise....In a pill?

08/02/2012 23:12

Peroxisome proliferator-activated delta (PPARδ ) control the transcription of genes involved in lipid metabolism. Activation of PPARδ may have antiatherogenic effects through the increase of plasma HDL, theoretically promoting reverse cholesterol transport from peripheral tissues toward the liver for removal via bile and feces. Effects of PPARδ activation by agonist GW1516 has been demonstrated to effectively reverse metabolic abnormalities in obese men with metabolic syndrome (a pre-diabetic condition), likely due to the fact that it stimulus fatty acid oxidation.

GW1516 holds promise for treating obesity and adiposity and has been touted, much like AICAR, as "exercise in a pill," etc. In conjunction with AICAR, an AMPK agonist which acts synergistically with GW1516, significant increases in exercise endurance have been demonstrated in animal studies.

GW1516 and AICAR are becoming popular items in the bodybuilding grey market. My approach here is try to mimic the effects of the combo termed exercise in a pill using supplement available in the market. Here are some of of the substances that can potentially work in a similar manner:

Potential PPARδ agonist or activators (GW1516 mimcers):

1) Tetradecylthioacetic acid (TTA): TTA is a non-selective PPAR agonist similar to GW1516 it activates PPARδ (weaker/less affinity) All three rodent peroxisome proliferator-activated receptor (PPAR) subtypes were activated by TTA in the ranking order PPARalpha > PPARdelta > PPARgamma. TTA is a non-beta-oxidizable fatty acid analog, which potently regulates lipid homeostasis.

2) Arachidonic acid (AA): PPARs are activated by their ligands, among which are arachidonic acid and other PUFAs (polyunsaturated fatty acids) , NSAIDs and cyclopentenone PGs. There are at least three PPARs, PPARα, PPARδ and PPARγ, of which the PPARα and PPARδ isoforms. Therefore activation of a PPAR is one mechanism by which arachidonic acid may induce PTGS2.
3) Sessamin and fish oil: Sesamin acts primarily as a ppar-agonist of the alpha type, but there is evidence that it maybe a weak activator of of other PPAR subtypes

Potential AMPK agonist (AICAR mimcers):

1) Forskolin: Is unique in its ability to stimulate adenylate cyclase activity and increasec AMP which regulates and activates critical enzymes required for the cellular energy. Long-term forskolin stimulation induces AMPK activation similar to AICAR
2) Methylxanthines: It is a competitive nonselective phosphodiesterase inhibitors which raise intracellular cAMP, activate PKA, inhibit TNF-alpha and leukotriene This is found in CL popular supplement White flood.

Other potential candidates: berberine, Caffiene, Alisma plantago aquatica (ze xie/european waterplantain), Catharanthus roseus (madagascar periwinkle), Acorus calamus (sweet calamus), Euphorbia balsamifera (balsam spurge), Jatropha curcas (barbados nut), Origanum majorana (marjoram), Zea mays (corn silk), Capsicum frutescens (chilli) and Urtica dioica (stinging nettle).