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Miscellaneous

Latest discoveries in prostaglandin receptor modulators

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Pages 1225-1235 | Published online: 25 Feb 2005
 

Abstract

Prostanoids (prostaglandins and the thromboxanes) are cyclooxygenase products derived from C-20 unsaturated fatty acids. Since arachidonic acid is the most abundant among these precursor fatty acids in mammals, including humans, the series 2 prostanoids are predominantly formed in the body. Thus, cyclooxygenases metabolise arachidonate to five primary prostanoids: PGE2, PGF2 α, PGI2, TXA2 and PGD2. These lipid mediators interact with specific members of a family of distinct G-protein-coupled prostanoid receptors, designated EP, FP, IP, TP and DP, respectively. As a review focused on latest discoveries and developments of novel TXA2 modulators patented from January 1997 to December 2000 has been recently published, this paper specifically focuses on newly developed IP, DP, FP and EP modulators patented for three years, from January 1998 to December 2001. Indeed, because prostaglandins are involved in a large series of pathophysiological processes, a classification of these modulators has been proposed, based on the type of receptors activated or inhibited. Their pharmacological profile is also described.

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