Autacoid Drugs ·Autacoids(自体活性物质)are biological factors made in the body that act like"local hormones", have a brief duration,act near the site of synthesis (paracrine),and are not blood borne. Autacoids are regulating molecules metabolized locally. These factors can have many different biological actions. Major autacoids ·Arachidonic acid metabolites(花生四烯酸) including:prostaglandins(前列腺素)， thromboxanes(血栓素)，leukotrienes(白三烯) ·5-hydroxytryptamine,5-HT(五羟色胺)，also named serotonin(血清素) ·Bradykinin(缓激肽) ·Endothelin(内皮素) Substance P(P物质)
Autacoid Drugs • Autacoids (自体活性物质) are biological factors made in the body that act like “local hormones”, have a brief duration, act near the site of synthesis (paracrine), and are not blood borne. • Autacoids are regulating molecules metabolized locally. • These factors can have many different biological actions. Major autacoids • Arachidonic acid metabolites (花生四烯酸) including：prostaglandins (前列腺素), thromboxanes (血栓素), leukotrienes (白三烯) • 5-hydroxytryptamine, 5-HT (五羟色胺）,also named serotonin (血清素) • Bradykinin (缓激肽) • Endothelin (内皮素) • Substance P (P 物质)
Synthesis of Eicosanoids(二十烷类) 777777 4… Phospholipase Ae Arachidonic acid 5-Lpox闪ygenase Prostaglandin G2 5-HPETE Prostaglandin H2 Leukotriene A Prostaglandin l2 Prosta Prostaglandin F2o Leukotriene Da Leukotriene E Arachidonic Acid (AA) (5.8.11.14 eicosatetraenoic acid) COOH 入CH3 .20 carbon,unsaturated fatty acid .Gives rise to PGs,thromboxanes and leukotrienes .Phospholipase A2(PLA2)and phospholipase C(PLC)generate AA from phospholipids and diacylglycerols .Fatty acid cyclooxygenases(COX-1 and COX-2)initiate the biosynthesis of the PGs and TXs(prostanoids) .Various lipoxygenases give rise to leukotrienes and lipoxins (inhib.of lipoxygenase are potential anti-asthmatic drugs)
Synthesis of Eicosanoids (二十烷类)
977779 4688 Phospholipase A2+ Injury or other stimulus Arachidonic acid Cyclooxygenase 5-Lipoxygenase (COX) Prostaglandin G2 5-HPETE Prostaglandin H2 Leukotriene A4 Prostaglandin 12 Prostaglandin E2 Thromboxane A2 Leukotriene B4 Leukotriene Ca Prostaglandin F2 Leukotriene D4 Leukotriene E 贝前列素Beraprost Beraprost is a synthetic analogue of prostacyclin.under clinical trials for the treatment of pulmonary hypertension.It is also being studied for use in avoiding reperfusion injury. As an analogue of prostacyclin PG12,beraprost effects vasodilation,which in turn lowers the blood pressure.Beraprost also inhibits platelet aggregation,though the role this phenomenon may play in relation to pulmonary hypertension has yet to be determined
贝前列素 Beraprost As an analogue of prostacyclin PGI2, beraprost effects vasodilation, which in turn lowers the blood pressure. Beraprost also inhibits platelet aggregation, though the role this phenomenon may play in relation to pulmonary hypertension has yet to be determined. Beraprost is a synthetic analogue of prostacyclin, under clinical trials for the treatment of pulmonary hypertension. It is also being studied for use in avoiding reperfusion injury
前列地尔Alprostadil Prostaglandin E1 (PGE1),known pharmaceutically as alprostadil,is a prostaglandin.It is a drug used in the treatment of erectile dysfunction[2]and has vasodilatory properties. 依前列醇Epoprostenol Prostacyclin(or PGI2),as a drug,is known as 'epoprostenol".The terms are sometimes used interchangeably. Prostacyclin(PGI2)chiefly prevents formation of the platelet plug involved in primary hemostasis (a part of blood clot formation).It does this by inhibiting platelet activation.It is also an effective vasodilator.Prostacyclin's interactions in contrast to thromboxane(TXA2),another eicosanoid,strongly suggest a mechanism of cardiovascular homeostasis between the two hormones in relation to vascular damage
前列地尔 Alprostadil Prostaglandin E1 (PGE1), known pharmaceutically as alprostadil, is a prostaglandin. It is a drug used in the treatment of erectile dysfunction[2] and has vasodilatory properties. 依前列醇 Epoprostenol Prostacyclin (or PGI2), as a drug, is known as "epoprostenol". The terms are sometimes used interchangeably. Prostacyclin (PGI2) chiefly prevents formation of the platelet plug involved in primary hemostasis (a part of blood clot formation). It does this by inhibiting platelet activation. It is also an effective vasodilator. Prostacyclin's interactions in contrast to thromboxane (TXA2), another eicosanoid, strongly suggest a mechanism of cardiovascular homeostasis between the two hormones in relation to vascular damage
米索前列醇Misoprostol HO Pharmacologically,misoprostol is a synthetic prostaglandin E1(PGE1)analogue. Misoprostol is a drug that is used for the prevention of non steroidal anti inflammatory drug (NSAID)induced gastric ulcers,for early abortion,to treat missed miscarriage,and to induce labor.The latter use is controversial in the United States.Misoprostol was invented and marketed by G.D.Searle Company (now Pfizer)under the trade name Cytotec. 地诺前列酮Dinoprostone,PGE2 OH HO OH The naturally occurring prostaglandin E2(PGE2)is known in medicine as dinoprostone.It has important effects in labor(softens cervix and causes uterine contraction)and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts.PGE2 is also the prostaglandin that ultimately induces fever
米索前列醇 Misoprostol Pharmacologically, misoprostol is a synthetic prostaglandin E1 (PGE1) analogue. Misoprostol is a drug that is used for the prevention of non steroidal anti inflammatory drug (NSAID) induced gastric ulcers, for early abortion, to treat missed miscarriage, and to induce labor. The latter use is controversial in the United States. Misoprostol was invented and marketed by G.D. Searle & Company (now Pfizer) under the trade name Cytotec. 地诺前列酮 Dinoprostone, PGE2 The naturally occurring prostaglandin E2 (PGE2) is known in medicine as dinoprostone. It has important effects in labor (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts. PGE2 is also the prostaglandin that ultimately induces fever