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Pump Spray - Triacetyladenosine

Adenosine is an important molecule that serves a wide variety of roles in the function of cells throughout the body.  You may be familiar of it as a component of adenosine triphosphate (ATP), which is the energy transfer molecule that keeps our body and brains working.  You may also have heard of cyclic AMP, which is a cellular messenger that carries the signal for such things as adrenaline to fat and muscle.   Less well known though is the fact that adenosine itself is a very important signaling molecule, especially in regards to blood flow.  In particular (and of most interest to us) is the effect of adenosine on blood flow to muscles.

Adenosine Compound Structure

When muscles are exercised, ATP starts to become depleted.  This cascade of depletion leads first to adenosine diphosphate (ADP), then to adenosine monophosphate (AMP), and finally to free adenosine.  This free adenosine formed is then released from the muscle during contraction under conditions of low pH (as lactic acid accumulates).  Outside the muscle it then interacts with adenosine receptors on the surface of the muscle cell, the neuromuscular junction, as well as the capillaries that feed the muscle.  Adenosine serves to open up the capillaries to help the working muscle stay supplied with nutrients and oxygen, as well as to take away metabolic waste products.  Additionally, adenosine’s interactions with its receptors on the muscle cell initiates what is known as the exercise mediated stimulation of glucose uptake.  The muscle cells thereby take in and process glucose rapidly directly – without the presence of insulin being required.

The effect of adenosine on muscular blood flow is well recorded and is dramatic.  Infusions of adenosine have been shown to increase blood flow and glucose uptake in skeletal muscle several fold.   This happens very rapidly.  Adenosine however must be infused into the blood stream since it is such a rapidly metabolized compound.  In fact, its half-life is less than ten seconds.  This is due primarily to the action of an enzyme called adenosine deaminase.  This enzyme irreversibly converts adenosine to a compound known as inosine.

  Adenosine Deaminase Compound Structure

The unstable nature of adenosine is unfortunate, as it makes its administration for physique and exercise enhancement problematic.  Some have tried to overcome this by offering it in the form of ATP, however this does not really solve the problem because once it is converted to adenosine (and this happens rapidly during digestion) it once again becomes susceptible to adenosine deaminase and much of it is destroyed.  Very little of it reaches the muscles.

We can protect adenosine from this rapid and destructive deamination reaction.   By making one of the hydroxyl groups (5’) on the ribose portion of the molecule into an ester, it has been found that the action of adenosine deaminase is blocked.  The protection of this hydroxyl group allows the compound extended lifetime in the body, so that it may reach target tissues.  Esterases at target tissues then regenerate the parent adenosine, where it may then interact with the appropriate adenosine receptors and impart its valuable pharmacological properties.

Epharm has chosen to use the acetate ester for protection of adenosine.   For purposes of convenience all three hydroxyl groups are made into acetates, and the end product is called triacetyladenosine.  Utilization of the ester form has an additional benefit, as it renders the compound soluble in organic solvent bases.  This allows it to be suitable for use in a topical formula, and that is exactly what we decided to do with Pump Spray.

Triacetyladenosine Compound Structure

By optimizing the influence of adenosine on the skeletal muscle you can achieve maximum capillary vasodilation.  This is manifested in what is known as exercise induced hyperemia, or more commonly referred to as “the pump”.  Adenosine does more than just allow for vasodilation in the muscle however, it also is known to mediate the exercise induced secretion of vascular endothelial growth factor (VEGF).  This growth factor serves the purpose to promote the formation of new capillaries, thereby augmenting the vascular network that feeds muscles for contraction as well as new growth.

Below are just a sample of references to just a few of the many articles published on the role of adenosine in muscle and exercise induced hyperemia.  It is clearly apparent that adenosine plays a key role in the physical response to exercise, and with the introduction of triacetyladenosine as a component of Pump Spray you are finally able to capitalize fully on its potential!!

Acta Physiol Scand. 2001 Feb;171(2):177-85.
Role of adenosine in exercise-induced human skeletal muscle vasodilatation.
Rådegran G, Calbet JA.

Acta Biochim Pol. 2006;53(2):269-78. Epub 2006 Jun 12.
Adenosine as a metabolic regulator of tissue function: production of adenosine by cytoplasmic 5'-nucleotidases.
Borowiec A, Lechward K, Tkacz-Stachowska K, Składanowski AC.

Hypertension. 2009 Jun;53(6):993-9. Epub 2009 May 11.
Adenosine contributes to blood flow regulation in the exercising human leg by increasingprostaglandin and nitric oxide formation.
Mortensen SP, Nyberg M, Thaning P, Saltin B, Hellsten Y.

J Appl Physiol. 2006 Aug;101(2):492-9. Epub 2006 Apr 13.
Bimodal distribution of vasodilator responsiveness to adenosine due to difference in nitric oxidecontribution: implications for exercise hyperemia.
Martin EA, Nicholson WT, Eisenach JH, Charkoudian N, Joyner MJ.

J Appl Physiol. 2010 Feb;108(2):378-86. Epub 2009 Nov 25.
Comparison of exogenous adenosine and voluntary exercise on human skeletal muscle perfusionand perfusion heterogeneity.
Heinonen I, Kemppainen J, Kaskinoro K, Peltonen JE, Borra R, Lindroos MM, Oikonen V, Nuutila P, Knuuti J, Hellsten Y, Boushel R, Kalliokoski KK.

Am J Physiol Heart Circ Physiol. 2010 Sep;299(3):H857-62. Epub 2010 Jun 11.
Contraction-induced secretion of VEGF from skeletal muscle cells is mediated by adenosine.
Høier B, Olsen K, Nyberg M, Bangsbo J, Hellsten Y.

Am J Physiol Regul Integr Comp Physiol. 2012 Feb 1;302(3):R385-90. Epub 2011 Nov 30.
Effects of adenosine, exercise, and moderate acute hypoxia on energy substrate utilization of human skeletal muscle.
Heinonen I, Kemppainen J, Kaskinoro K, Peltonen JE, Sipilä HT, Nuutila P, Knuuti J, Boushel R, Kalliokoski KK.

Am J Physiol Regul Integr Comp Physiol. 2005 Aug;289(2):R283-R296.
Growth regulation of the vascular system: an emerging role for adenosine.
Adair TH.

Hypertension. 2010 Dec;56(6):1102-8. Epub 2010 Nov 1.
Interstitial and plasma adenosine stimulate nitric oxide and prostacyclin formation in humanskeletal muscle.
Nyberg M, Mortensen SP, Thaning P, Saltin B, Hellsten Y.

J Physiol. 2001 Nov 1;536(Pt 3):927-35.
Oxygen delivery and oxygen consumption in rat hindlimb during systemic hypoxia: role ofadenosine.
Edmunds NJ, Marshall JM.

J Appl Physiol. 2007 Dec;103(6):2042-8. Epub 2007 Sep 20.
Role of adenosine in regulating the heterogeneity of skeletal muscle blood flow during exercise inhumans.
Heinonen I, Nesterov SV, Kemppainen J, Nuutila P, Knuuti J, Laitio R, Kjaer M, Boushel R, Kalliokoski KK.

Adv Exp Med Biol. 1998;441:97-106.
Role of adenosine in regulation of carbohydrate metabolism in contracting muscle.
Hespel P, Richter EA.

J Physiol. 2007 Sep 15;583(Pt 3):835-45. Epub 2007 Jul 5.
The roles of adenosine and related substances in exercise hyperaemia.
Marshall JM.

Am J Physiol Heart Circ Physiol. 2010 Sep;299(3):H857-62. Epub 2010 Jun 11.
Contraction-induced secretion of VEGF from skeletal muscle cells is mediated by adenosine. 
Høier B, Olsen K, Nyberg M, Bangsbo J, Hellsten Y.



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