Group,

This is a very complex subject, but it has received a lot of attention lately regarding skin inflammation and inflammatory pain.... both centrally in the CNS and Peripherally in the skin.

NMDA is a receptor that is involved in many functions. One of the main pathogenic functions is flushing, inflammation and pain syndromes. There is an oral drug out called Namenda being used for various disorders including inflammatory skin disorders such as Psoriasis and Lupus... but with GREAT caution. I am not recommending this treatment, just posting the latest information and research that is directly pertinent for rosacea, especially neurovascular rosacea with chronic flushing, inflammation and pain (centrally modified over time AND peripherally in the pain nerve endings of the skin). NMDA receptor involvement in rosacea was brought up at the latest International Dermatology Meeting in 2009.

In addition to the oral NMDA blocker, there are over a dozen companies working on anti-NMDA antibodies to irreversibly bind to the main subtype of NMDA receptor that is key to inflammation and pain. They can perform this topically and orally.

NMDA receptor illustration below shows that Magnesium and Glutamate (which many take for sleep, fibromyalgia and muscle aches) are strong activators of these receptors. You may want to discuss this with your physician, preferrably one with a strong biochemical and molecular background .



As this is still in the experimental stages with regards to rosacea and other inflammatory skin disorders, PLEASE DISCUSS ANY NMDA ANTAGONIST APPROACH WITH YOUR PHYSICIAN FIRST. You will find a lot of NMDA receptor information about memory and alzheimers, but our focus is on a different subclass of NMDA receptors.

There is one interesting supplement that shows surprising potential at blocking this receptor centrally which theoretically should reduce nerve hyperactivity that leads to flushing and neuropathic pain of facial skin:

Ions and amino acid analysis of Cyperus articulatus L. (Cyperaceae) extracts and the effects of the latter on oocytes expressing some receptors
Journal of Ethnopharmacology, Volume 95, Issues 2-3, December 2004, Pages 303-309

E. Ngo Bum, K. Lingenhoehl, A. Rakotonirina, H-R. Olpe, M. Schmutz and S. Rakotonirina

Extracts from rhizomes of Cyperus articulatus L. (Cyperaceae) used in Africa and Amazonia to treat many diseases has been shown to possess sedative and anticonvulsant properties. The aim of this study is to determine the mechanism of action of Cyperus articulatus extracts. In Xenopus oocytes expressing receptors, using electrophysiological measurement, extracts of rhizomes of Cyperus articulatus (300 ìg/ml) inhibited 50% of the EC50 and EC80 of glutamate (1.3 and 2.9 microM, respectively) induced inward current through hNMDAR1A/2A receptors. Extracts induced very small current through rGluR3 receptors. The largest current induced by the extract (30 mg/ml) represents 128% of the EC100 of glutamate induced inward current, through rGluR3 receptors. The excess 28% current could be induced by aspartate and/or glutamate in the extracts. The effect on Xenopus oocytes expressing heteromeric GABABR1b/R2 receptors and rectifying potassium channels (Kir3) is clear. A decoction and water extract of Cyperus articulatus induced a large inward current that represented 71 and 57% (respectively) of the EC100 of gaba (30 ìM) induced inward current. The water extract induced also a large current through rectifying potassium channels (Kir3). Part of the current induced through GABAB receptors could be related to rectifying potassium channels and GABAB site receptors. Cyperus articulatus extracts possessed components that could decrease excitation (NMDA receptor antagonists) and increase inhibition (GABAB receptor agonists) in the central nervous system.

If you've read this far, give yourself a gold star and take some aspirin. You will be quized on this on Friday.

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Best,
Geoffrey

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

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

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Interesting Dr. Nase. We compound various NMDA antagonists in our pharmacy. Sounds promising.

Do you have the information or abstracts from the Dermatology conference on this subject?