Pain & Inflammation

Nociception (pain perception) and inflammation are two responses of an organisms defence system towards external noxious stimuli. Although different in nature, pain and inflammation are strongly associated with each other. An important sign of inflammation - besides local redness, swelling, heat, and loss of function -  is in fact pain. The events of inflammation that underlie these symptoms are induced and regulated by a large number of chemical mediators that are also found to mediate the mechanisms of pain perception. These mediators include eicosanoids, kinins, complement proteins, neurotransmitters (e.g. histamine), protons, NO, prostaglandins, leukotrienes, neurotrophins, and monokines[1].
Inflammation is a major protective response of the immune system to tissue damage and infection, and ranges from the acute inflammation associated with infection of the skin, through to chronic inflammatory processes in atherosclerosis, asthma and chronic bronchitis, and rheumatoid arthritis, among many others. Acute inflammation is knows for its rapid onset and short duration. It is mediated by tissue-resident macrophages and mast cells, and characterized by the exudation of fluids and plasma proteins, and the migration of leukocytes (mainly neutrophils) into the injured area. In contrast, chronic inflammation is of a more prolonged duration and manifests histologically by the presence of lymphocytes and macrophages, resulting in fibrosis and tissue necrosis[2].
Similar to Inflammation, pain may also be divided into two main categories: acute and chronic pain. Acute or nociceptive pain is part of a rapid warning relay instructing the motor neurons of the central nervous system to minimize detected physical harm. It is mediated by nocicepters: free nerve endings that terminate just below the skin, in tendons, joints, and in body organs.  Nociceptors are extremely heterogeneous, differing in the neurotransmitters they contain, the receptors and ion channels they express, their speed of conduction, their response properties to noxious stimuli, and their capacity to be sensitized during inflammation, injury, and disease. Nociception can be associated with nerve damage caused by trauma, diseases such as diabetes, shingles, irritable bowel syndrome, late-stage cancer or the toxic effects of chemotherapy. It typically responds well to treatment with opioids and NSAIDs. Chronic pain, however, serves no biologic function as it is not a symptom of a disease process but is a disease process itself[3],[4].


[1] R. Medzhitov. Origin and physiological roles of inflammation. Nature 2008, 454, 428-435.
[2] E.O. Iwalewa et al. Inflammation: the foundation of diseases and disorders. A review of phytomedicines of South African origin used to treat pain and inflammatory conditions. Afr. J. Biotech. 2007, 6, 2868-2885.
[3] M. Percival. Understanding The Natural Management of Pain and Inflammation. Clin. Nutr. Insights 1999, 4, 1-5.
[4] C.L. Stucky et al. Mechanisms of pain. PNAS October 9, 2001, 98, 11845-11846.

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2062 Alprostadil Prostaglandin EP (1-4) receptor antagonist €105.00
2145 AZD 1981 Selective CRTH2 (aka DP2) antagonist €105.00
2788 ER-819762 Highly selective, and orally available PGE2 receptor EP4 antagonist  Recently added €155.00
2533 Hydroxypioglitazone Active metabolite of Pioglitazone (M-IV), a PPARγ agonist €235.00
1480 MK 0524 sodium salt PGD2 receptor DP1 antagonist €125.00
1913 OC 000459 Selective DP2 (CRTH2) antagonist €90.00
1512 ONO 8711 dicyclohexyl amine salt PGE1 receptor EP1 antagonist €120.00
2024 PF 04418948 Prostaglandin EP2 receptor antagonist €95.00
2020 PF 4693627 Selective and orally bioavailable inhibitor of mPGES-1 €125.00
2443 Rosiglitazone PPARγ agonist; antidiabetic drug and stem cell differentiator €95.00
1605 S 5751 PGD2 receptor DP1 antagonist €115.00
2605 Selexipag Prodrug of MRE 269, a potent IP receptor (PGI2) agonist €90.00

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