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Old 2nd September 2010, 03:56 PM
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Arrow ANTI-REDNESS & ANTI-FLUSHING TREATMENTS: V-101 and SansRosa Failures Continue

One of the main problems with rosacea treatment and research is that we have fallen into the medical abyss -- we have the wrong physicians treating us. To treat the core disturbances and not just cover up our superficial symptoms you need a team of experts such as Vascular Specialists, Physiologists, Pharmacologists and Molecular Biologists as this is not a "Skin Disorder". Skin changes and immune changes (e.g. the notorious Cathelicidins) occur secondarily, but the instigating events are all vascular in nature.

Dermatologists are the wrong physicians to be researching topical vasoconstrictors on rosacea patients and their 9-year failure with SansRosa is a prime example. They have not identified the two types of alpha adremoceptors they reside in the facial skin (e.g. alpha adrenoceptor-1 and alpha-adrenoceptor-2) and are only targetting alpha-1 adrenoceptors with large concentrations of topical, high molecular weight drugs.

You first need to understand the receptor distribution of alpha adrenoceptors in facial blood vessels (inner wall, middle wall and outer wall)) and stimulate BOTH receptor subtypes simultaneously for the best constrictor responses, the longest constriction and by targetting both receptor subtypes, the chances for rebound dilation are almost zero -- this is called alternate receptor stimulation and is well known to Vascular specialists. It does not allow one receptor subtype to get overwhelmed, overstimulated, overused, or "fight back" via rebound dilation phenomenon.

Plus in 9 years Galdema never once performed the most pivotal study to determine receptor subtypes in rosacea blood vessels (and V-101 is following the same dead end). There is most likely a third type of alpha adrenoceptor unaccounted for..... alpha adrenergic-3 receptor subtype and for our best possible treatment, specialists must research and identify the subtypes of each receptor class -- each receptor subtype contaiins three divisions and each one plays a different role (e.g. alpha 1a, alpha 1b, alpha 1c, alpha 2a, alpha 2b, alpha 2c and a whole new class of alpha subtype 3 receptors).

The research has been unremarkable and their continued failures become more evident. They simply got sloppy and did not ask for outside collaboration from Vascular Specialists. In reality, it would be quite simple to figure this mess out and get the best treatment to market fairly quickly. All you need are 20 to 30 biopsies from rosacea skin that contain various sizes of blood vessels (approximately 5 microns to 300 microns) and then send them off to a molecular biology lab to determine the exact types of receptors, number of receptors, and activity of each receptor analyzed... and then send them to a pharmacology drug lab to have the drugs tested on each receptor subtype so we know exactly how much constrictor to use and if we need a higher dose of alpha 2 receptor drug versus alpha 1 or vice versa. This is the absolute best, most scientific approach that takes out all the guesswork. You just don't squirt a constrictor on a rosacea patient's face for 9 years and see what happens..... that's why it took Galderma 9 years and they are still near gound zero.

We did a lot of bio-medical and drug research in this very area for my doctoral work at WVU School of Medicine and you can actually read one of the more important studies I published in the Journal of American Physiology [Heart and Circulatory Physiology 'Edition for the National Institutes of Health (NIH)] that covers this exact issue --it discusses how you determine what type of alpha receptors are present in blood vessels, their physiological and pharmacological actions, and their distribution in different areas of the body..... the most important thing to making a succesful rosacea treatment.

This is exactly what we are doing with our Rosadyn Topical right now and we see much better constriction, much longer constriction and NO rebound dilation.

You can read my peer reviewed medical journal online for free. It may help you understand all the past failures or it may put you to sleep:

Dr. Nase and Alpha Adrenoceptor Study

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Dr. Geoffrey Nase
Ph.D: Neuro-Vascular Physiologist

Email: drnase1000@hotmail.com
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Old 3rd September 2010, 12:24 AM
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Clin Exp Hypertens A. 1989;11 Suppl 1:21-30.

Alpha-adrenoceptor subtypes in blood vessels: physiology and pharmacology.
Langer SZ, Schoemaker H.

Abstract

The existence of alpha 1- and alpha 2-adrenoceptors subtypes is now well established. Presynaptically, alpha 2-adrenergic autoreceptors modulate norepinephrine release. In vascular smooth muscle both alpha 1- and alpha 2-adrenoceptors exist postjunctionally, the alpha 1 subtype being innervated preferentially in most vascular beds. alpha 2-Adrenoceptors may be present on the smooth muscle cell as well as the endothelial cell where they may participate in the release of endothelium derived relaxing and constricting factors. Developing insights into the role of alpha-adrenoceptor subtypes in the cardiovascular system, and into the classification of subtypes of alpha 1- and alpha 2-adrenoceptors may be expected to have, if confirmed, significant therapeutic implications for drug discovery in the cardiovascular system.

PMID: 2545380 [PubMed - indexed for MEDLINE]
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Dr. Geoffrey Nase
Ph.D: Neuro-Vascular Physiologist

Email: drnase1000@hotmail.com
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Old 3rd September 2010, 12:28 AM
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Default Back to G-Proteins

Once again we are back to the all-important G-Proteins:

Adrenergic receptor

From Wikipedia

Adrenaline

NoradrenalineThe adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines, especially noradrenaline (norepinephrine) and adrenaline (epinephrine). Although dopamine is a catecholamine, its receptors are in a different category.

http://en.wikipedia.org/wiki/Adrenergic_receptor

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Dr. Geoffrey Nase
Ph.D: Neuro-Vascular Physiologist

Email: drnase1000@hotmail.com
Bibliography: http://drnase.com

All posts are for informational purposes only. Please visit our Home Page to view our Medical Disclaimer.
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Old 7th September 2010, 09:53 AM
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Dr. Nase,

one can clearly see that you have a really huge knowledge about all this medical things PLUS you are sooo interested in finding a treatment that really helps us rosacea sufferes.

Go for it, find this treatment...or even better, a cure!

Thanks for all!

Barbara
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