Axon
Hederagenin
((3-beta,4-alpha)-3,23-dihydroxyolean-12-en-28-oic acid)
...There are many stimulants on the market -- but none of them are anything like this.
AXON is based on a triterpene known as "Hederagenin" -- extracted from Hedera Helix. This triterpene is a triple monoamine reuptake inhibitor: A high-affinity substrate for the dopamine, 5-HT, and norepinephrine neural membrane transporters. (DAT, SERT, and NET, respectively.) Before we expound on this specific function any further, a few general words on how these monoamine neurotransmitters work:
The human brain contains billions of neurons which release neurotransmitters. They all consist of a cell body (the soma) & a long chain (the axon) which connects via branches to other neurons. Transmission via the axon is how one cell can influence others, and this is often carried out via monoamines such as DA, NE, 5HT; in response to electrical stimuli, they are released from the axon terminal into the synaptic gap, where they seek out and bind to receptors on the other side of the gap, on other neurons. This binding is not permanent: most of these monoamines are shaken-off their receptors in a matter of milliseconds, and are then 'available' once again. Their function is terminated by monoamine reuptake from the synaptic cleft back into the neuron via membrane-bound transporter proteins. (Glycoproteins, typically.) Following reuptake, most are metabolized into inert derivatives, and some are recycled and re-released.
...As you can imagine, when reuptake proteins are inhibited, monoamine breakdown comes grinding to a halt and they start accumulating outside neurons -- eventually flooding synapses & increasing transmission to supraphysiological levels.
That's the whole point. Reuptake-inhibition makes for a powerful stimulant. Although Hederagenin has its mechanism of action in common with some banned chemicals, no ingredient previously released as a supplement is anything quite like it. Ephedrine, for example, is a potent NET inhibitor, but has an extremely weak effect on dopaminergic transmission and no effects at all where the serotogenic pathway is concerned.
By increasing dopaminergic, adrenergic, and serotogenic transmission, you get an increase in energy levels, heightened focus, an elevated mood, increased confidence and drive, and an revved-up metabolic rate.
And there is another interesting and potentially-useful effect: ***945;-hederin, a hederagenin saponin present in high quantities in Hedera Helix (and therefore AXON), prevents ***946;2-adrenoceptor internalization and desensitization. In doing so, it strongly increases the binding potential of these receptors to other ligands. It is therefore likely that AXON has a synergystic effect with compounds which target and bind to the ***946;2-adrenoceptor.
AXON can be stacked with other non-stimulant fat burners. It is completely safe for human consumption, and has been side-effect free in all of our testers.
Use as part of a weight-loss regimen, to increase performance and endurance in the gym, or for the long-lasting energy you need to cope with a busy work or study schedule.
Where pharmacokinetics are concerned:
Hederagenin is very lipophilic & nearly-insoluble in water. It is slowly and poorly absorbed from the GI tract, but the half-life & duration of effect of the absorbed fraction is long. (6-8+hrs.) As has been conclusively shown with another triterpene, boswelic acid, absorption and bioavailability will increase tremendously when taken with food.
Scientific data:
Binding affinity (as Ki):
SERT at cerebral cortex: 3.89±0.18 nm
NET at hypothalamus: 0.22±0.04 nm
DAT at striatum: 2.87±0.54 nm
(NET>DAT>SERT, though very high affinity for all three.)
Affinity for other neural receptors:
Selective for NET, DAT, and SERT. No affinity for: D1, D3, D2, D4, D5, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2a, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6, 5- HT7, ***945;1A, ***945;1B, ***945;2A, ***946;1, M1, M2, M3, M4, M5, ***956;, ***954;, ***948;, A1, A2A, H1, H2, H3, H4.
(Of course, the D, 5-HT, and alpha/beta receptors are affected downstream, as a result of this aforementioned DAT, SERT, and NET inhibition.)
Solubility:
Effectively insoluble in water (0.34 mg/L)
Slowly but appreciably soluble in ethanol, isopropanol, methanol and pyridine.
LogP:
7.41 (extremely lipophilic)
These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure or prevent any disease.
Patent Pending.
References:
1. Jin ZL, Gao N, Zhou D, Chi MG, Yang XM, Xu JP. The extracts of Fructus Akebiae, a preparation containing 90% of the active ingredient hederagenin: serotonin, norepinephrine and dopamine reuptake inhibitor. Pharmacol Biochem Behav. 2012;100(3):431-9.
2. Wolf A, Gosens R, Meurs H, Häberlein H. Pre-treatment with ***945;-hederin increases ***946;-adrenoceptor mediated relaxation of airway smooth muscle. Phytomedicine. 2011;18(2-3):214-8.
3. Sterk V, Büchele B, Simmet T. Effect of food intake on the bioavailability of boswellic acids from a herbal preparation in healthy volunteers. Planta Med. 2004;70(12):1155-60.
