Agmatine is decarboxylated argenine. Argenine, a common amino acid, and agmatine are both found naturally in the body. Agmatine is found in small vesicles near the opposing surface of a nerve synapse. It is one of the new neuromodulators being studied.
A considerable amount of very significant pain research has come from the University of Minnesota. One of the more recent articles is by Goracke-Postle et al in Neuroreport. 2006 Jan 23;17(1):13-7.
By now, you have likely come to understand that the structure of proteins is VERY important in nervous function, and is very sensitive to the pH of the environment. Some feel that perineural acidosis is really what is behind central pain. The body combines MANY compounds in making things more acid, since pH is one of the closely controlled things in the body, because pH is so potent in changing the shape, and hence the function, of proteins.
You should also have learned that most proteins are made of amino acids and the resulting protein molecule is huge by comparison. Chains of amino acids of less than two hundred units are called peptides. You can think of peptides as mini-proteins. Small portions of the molecules of proteins and peptides are exposed to outside chemical bonding. Much of the molecule is ordinarily hidden or concealed by shape and the bonding angles of atoms which can prevent such things as water from entering the structure.
Changes in pH may expose or conceal certain parts of the protein. These modified parts may include certain sequences of amino acids which act as receptors for some other neuroactive chemical. This chemical, when it binds, may alter the protein, creating binding opportunities or destroying access by other chemicals. Structure and configuration have thus become VERY important in the world of molecular pain studies. The channels through which ions must pass to create an action potential (or neuron firing) are made of proteins. Channel characteristics and behavior are very much the result of the amino acids of which they are comprised.
One of the common amino acids in humans is arginine. When a COOH (carboxyl group of carbon, two oxygens and one hydrogen) group is removed (decarboxylated)the arginine becomes agmatine. This substance occurs naturally in the body. The researchers mentioned above used tritium, which is a type of Hydrogen which is easily measured, to label agmatine and found it to be closely associated with synaptotagmin and synaptophysin, two molecules closely associated with nerve synapses. The small packets in which chemicals are found near the synapse are sometimes called “synaptosomes”. This is where agmatine can be found naturally.
It now appears that agmatine can reduce pain. Currently, it is given intrathecally, which means into the spinal fluid, just as Prialt is. However, agmatine should be, at least theoretically, very inexpensive. Amino acids are generally cheap and removing a carboxyl group is a cinch for organic chemists.
It is possible this substance may find a use in the treatment of chronic pain. Agmatine is released through the influence of Calcium. The calcium channels are complicated and discussed elsewhere at this site in multiple articles. We hope to see a role for agmatine in humans. It seems likely to be extremely safe, but then you never really know until tests have been run. Even table salt and sugar must be given in the proper amounts to humans.