Agmatine et douleur

Agmatine is an amine synthesized by L-arginine decarboxylation found in the central nervous system (CNS). Because of its mode of synthesis, storage in synaptic vesicles, and release and uptake mechanisms, agmatine is an important neurotransmitter involved in pain processing. In animal models, agmatine has antihyperalgesic and antiallodynic activity in chronic rather than acute pain. Mechanisms involve the activation of imidazoline and alpha2-adrenergic receptors, blockade of N-methyl-D-aspartate receptor channels and other ligand-gated cationic channels, and inhibition of nitric oxide synthase activity. In animal studies, agmatine potentiates morphine analgesia without directly interacting with opioid receptors and reduces tolerance, dependence and withdrawal by interacting with intracellular cyclic adenosine monophosphate (cAMP) signaling. The discovery of new targets may provide a better understanding of its physiological role. These data allow consideration of agmatine as a potential therapeutic agent in the management of chronic pain alone or combined with low doses of opiate analgesics.