Vialox? (pentapeptideamide-4)

[Dee]

Dr. Todorov,
Can you tell me what Vialox is? From what I've read it's a curare-like alternative to botox. I've only heard about it this week as it's now being sold in products as a topical muscle relaxer similar to Argireline only apparently more effective. It is manufactured by Pentapharm. Is it a new product or an old one? Is it safe and do you know what percentage it has been tested at? And mostly, is it effective???

[drtodorov]

Don't know this brand, sorry. These rub-on "Botox alternatives" are multiplying like rabbits :)

[claire63]

Did you ever try a Vialox product, Dee? I tried the Relax Plus with Vialox starting last May when it came out and I'm still using it on my frown lines. It is definitely stronger than acetyl hexapeptide though I still use that on my crow's feet since it is cheaper.

[Dee]

Yes I did try it but it did nothing for me. I guess I'm one of those people who just doesn't get any results from these botox-like topicals.

[claire63]

When I talked to the customer service rep at Cellular skin rx, she told me if you don't make alot of something called acetacolamines? sp? then the acetyl hexapeptide 3 won't work as well. She said that one out of about every 10 people just don't make that much of it. So maybe you are one of those.

The Vialox doesn't work the same way though. No acetyl hexapeptide in it. I do find I have to use it twice a day as they say or my results will fade out and the muscles seem to get moving again.

[drtodorov]

I presume she means 'catecholamines', which are a class of neurotransmitters, such as norepinephrine.

[merton]

I believe she means "acetylcholine". This product is an nicotinic acetylcholine receptor antagonist. At the post-synaptic site it selectively binds to its particular receptor and causes charged sodium ions to cease being released which causes depolarization (cessation of electrical charge) and thus the electrical pulse which causes the wrinkle. This is an action mimicking the blow-dart toxin, Curare.

Its probably an alpha isomer of a conotoxin but possibly a mu isomer (from one of many types of shellfish or alpha-bungarotoxin from the formosian cobra.) These are my tenative conclusions after much research. The manufacturer has made it quite difficult to pinpoint which is of course their right. Its not a pentapeptide-amide as the INCI name would logically indicate. here's a few of the hundreds of articles none of which deal with wrinkles:

http://www.jbc.org/cgi/content/abstract/272/39/24279?ijkey=221191207194907313fc40d5f6c798cbb9220f98&keytype2=tf_ipsecsha

http://grimwade.biochem.unimelb.edu.au/cone/vencomp.html

This is the first of two acetylcholine receptor antagonist products on the market for wrinkles.

I'd expect to see many more in the near future.

[drtodorov]

If this is indeed its purported mechanism of action, it may have aproimately oposing effect to DAME, which supposedly potentiates cholinergic effects.

[merton]

Hi Dr. Todorov,

Your reply is coming while I was still editing the above.

Yes, DMAE seems to be an aceytlcholine receptor agonist, as opposed to antagonist, which seems to preclude the indication of using DMAE with argireline(tm) concommitantly for the same reason, (although I find the product cited above (Vialox(tm) to be singnificantly more impressive in result - the same company makes both). I recall this comparison from your infopacks.

The second available such item now on the market, for reasons unknown, is substantially easier to get close to identifying, although its a synthetic 22 peptide long molecule for which published mutagens have been published (at the #5 position in the sequence) which reduce its toxicity. Its based on Waglerin 1 from the Temple Viper, Tropidolaemus wagleri.

[here's an example where Aspartic Acid(D) is being replaced with Glutamic Acid(E) and then alternatively with Asparagine(N) to yeild mutagens of the 22-peptide sequence of the Temple Viper's WAG-1 venom component, yeilding a "slight decrease in lethality".

http://ca.expasy.org/cgi-bin/sprot-ft-details.pl?P24335@MUTAGEN@5@5

Perhaps the large number of varients allows a bit more comfort towards disclosure and enough time until release of the next].

Here's some pictures of this ant-wrinkle creature:

http://www.kingsnake.com/viper/

Being a Swiss product (with the snake farm in Brazil) the Swiss-Prot engine seems to be most up to date). The articles refered to can be obtained in full length by googling title's if there's difficulty directly accessing them from here.

http://ca.expasy.org/uniprot/P24335

My experience with the item refered to in the previous post (Vialox(tm) has been impressive.

Its (Vialox(tm) packaging is just as impressive being finished at the manufacturer and requiring two components to be screwed together to reconstitute. Presumably this is because of the toxic nature of the contents. This packaging would be great for items like egf.

-merton

[drtodorov]

Well, the desire to come up with a rub-on Botox alernative is legitimate, but this is bumpy road.

P.S. What's your background - something science/medicine related? Just curious...

[merton]

Please see email.

This is another good article that describes sequencing and some enlargable illustrations of some of these nAChR antagonists. Note that another subdivision beyond the isomers I've mentioned are neronal and muscular versions. Also, some affect Na+ ion channels, some the K+ ion channel and others the Ca2+ ion channels. Both wrinkle products to date affect the Na+ channel specifically:

http://content.febsjournal.org/cgi/content/full/264/2/281

[guapagirl]

Hi Merton and Dr Todorov

For the thickies amongst us (OK, I mean me!), can you clarify that using DMAE and Agireline / vialox is counterproductive?

cheers, Liz 8)

[drtodorov]

Basically, DMAE increases muscle and possibly skin tension by indirectly activating cholinergic receptors. Vialox, allegedly, blocks such receptors, and thus may act in opposing direction.

[guapagirl]

Thanks Doc, so does agireline act in the same way? I am thinking of restocking but won't if it will be counteracted by my DMAE.

Thanks, Liz 8)

[merton]

The simple answer would be that wrinkles are caused by constant electrical pulses via nerves to the muscles which keeps them tense. There are gaps in the electric wires (nerves) called synapses. For the electricity to get across these synaptic gaps they use ferry boats called neurotransmitters which can only doc at their port on the other side. If that port is blocked the neurotransmitter can't drop off its passenger, electricity. Argireline blocks the port of the neurotransmitter called norepinephine. It can't drop off the electricity so there's no mucle contractions and therefore no wrinkles. It works by relaxing the muscle by deprieving it of electricity. The operative word here is "relax".

Another neurotransmitter (ferryboat) is called acetylcholine (which is abundant in soya lechitin and egg whites). Rather than decrease electricity DMAE increases the speed and number of ferryboats (acetylcholine) so more electricity gets across causing more muscle contractions which has the expected result of tensing (opposite of relax) the underlying muscles. This causes the skin to tighten (and make one smarter - DMAE/acetylcholine's better known property - Alzheimer's is characterized by diminished acetylcholine).

So relaxing and tensing at the same time would be a somewhat useless endeavor. So don't apply argireline and DMAE at the same time in the same place. Argireline and definitely not the above-toxins should not be placed below the eye or on the neck because of sag. DMAE is the more logical choice here.

And as the infopack points out DMAE may go beyond tightening the neck "skin" after time and remove the underlying "sag" or "gobbler".

[Another apparent sychronicious simultaneous transmission Dr. T - 2x in 24 hours]

-merton