- 関
- prostaglandin inhibitor
WordNet
- a drug that neutralizes or counteracts the effects of another drug
- a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
- a potent substance that acts like a hormone and is found in many bodily tissues (and especially in semen); produced in response to trauma and may affect blood pressure and metabolism and smooth muscle activity
PrepTutorEJDIC
- 対立する人,敵対者,競争相手(opponent)
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/12/12 12:04:34」(JST)
[Wiki en表示]
A Prostaglandin antagonist is a hormone antagonist acting upon prostaglandin.
NSAIDs inhibit cyclooxygenase and reduce prostaglandin synthesis. Corticosteroids inhibit phospholipase A2 production by boosting production of lipocortin, an inhibitor protein. Relatively new drugs, known as COX-2 selective inhibitors or coxibs, are used as specific inhibitors of COX-2. The development of these drugs allowed the circumvention of the negative gastrointestinal effects while effectively reducing inflammation.
Contents
- 1 Adverse effects
- 2 See also
- 3 References
- 4 External links
Adverse effects[edit]
Both NSAIDs and Coxibs can raise the risk of myocardial infarction, when taken on a chronic basis for at least 18 months. One emerging hypothesis that may explain the cardiovascular effects is that coxibs create an imbalance in circulating TxA2 (thromboxane) and PGI2 (prostacyclin) levels. An increased in the ratio of TxA2/PGI2 could lead to increased platelet aggregation and dysregulation of platelet homeostasis.[1]
See also[edit]
Mechanism of action of aspirin
References[edit]
- ^ Cheng Y et al., Role of prostacyclin in the cardiovascular response to thromboxane A2. “Science” 2002;296:539-51. PMID 11964481.
External links[edit]
- Prostaglandin antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
Receptor antagonists: hormone antagonists
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Hypothalamic/pituitary axes |
Adrenal axis:
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- Corticotropin releasing hormone antagonists
- Glucocorticoid antagonists
- Mineralocorticoid antagonists
- Selective glucocorticoid receptor agonist
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Thyroid axis:
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Gonadal axis:
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- Androgen antagonists
- Antigonadotropins
- Estrogen antagonists
- Gonadotropin-releasing hormone antagonists
- Progesterone antagonists
- Selective androgen receptor modulator
- Selective estrogen-receptor modulator
- Selective progesterone receptor modulator
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Eicosanoid |
- Leukotriene antagonists
- Prostaglandin antagonists
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Other |
- Cholecystokinin antagonists
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UpToDate Contents
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English Journal
- Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection.
- Vito VD1, Saba A2, Lee HK3, Owen H4, Poapolathep A5, Giorgi M6.
- Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2016 Jan 25;118:251-8. doi: 10.1016/j.jpba.2015.11.004. Epub 2015 Nov 7.
- Grapiprant, a novel pharmacologically active ingredient, acts as a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). It is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis. The aim of
- PMID 26580822
- Microsomal Prostaglandin E Synthase-1-Derived PGE2 Inhibits Vascular Smooth Muscle Cell Calcification.
- Gao C1, Fu Y1, Li Y, Zhang X, Zhang L, Yu F, Xu SS, Xu Q, Zhu Y, Guan Y, Wang X, Kong W.
- Arteriosclerosis, thrombosis, and vascular biology.Arterioscler Thromb Vasc Biol.2016 Jan;36(1):108-21. doi: 10.1161/ATVBAHA.115.306642. Epub 2015 Nov 5.
- OBJECTIVE: Chronic administration of selective cyclooxygenase-2 (COX-2) inhibitors leads to an increased risk of adverse cardiovascular events, including myocardial infarction and stroke. Vascular smooth muscle cell (VSMC) calcification, a common complication of chronic kidney disease, is directly r
- PMID 26543101
- Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
- Blanco MJ1, Vetman T2, Chandrasekhar S2, Fisher MJ2, Harvey A2, Mudra D2, Wang XS2, Yu XP2, Schiffler MA2, Warshawsky AM2.
- Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2016 Jan 1;26(1):105-9. doi: 10.1016/j.bmcl.2015.11.023. Epub 2015 Nov 10.
- A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was identified. Selectivity and pharmacokinetic profi
- PMID 26608552
Japanese Journal
- Industrial Info. プロスタグランジン受容体選択的作動薬の研究開発
- ヒト歯髄培養細胞におけるplasminによるcalcineurinを介したCOX-2発現
- 神尾 直人,室町 幸一郎,葉山 朋美,岡部 達,神尾 素代,諸橋 利朗,松島 潔
- 日本歯科保存学雑誌 57(5), 442-451, 2014
- 目的 : Plasminは細胞外基質成分の消化だけでなく前駆体MMPsの活性化にも関与し, 線維素溶解・炎症・組織修復にかかわる生理学的・病理学的にも重要なセリンプロテアーゼである. また近年, plasminは細胞膜上に存在するprotease activated receptors (PARs) を介して炎症シグナルを伝達する報告がある. 著者らはそれが歯髄炎の進行にも関与していると考え, …
- NAID 130004716690
- Exacerbation of Intracranial Aneurysm and Aortic Dissection in Hypertensive Rat Treated With the Prostaglandin F–Receptor Antagonist AS604872
- Fukuda Miyuki,Aoki Tomohiro,Manabe Toshiaki [他],Maekawa Akiko,Shirakawa Takayuki,Kataoka Hiroharu,Takagi Yasushi,Miyamoto Susumu,Narumiya Shuh
- Journal of Pharmacological Sciences 126(3), 230-242, 2014
- … Given the involvement of prostaglandin F2α and its receptor, FP, in extracellular matrix remodeling in a mouse model of pulmonary fibrosis, here we induced hypertension and IA in rats by salt loading and hemi-lateral ligation of renal and carotid arteries and examined effects of a selective FP antagonist, AS604872, on these vascular events. …
- NAID 130004700281
Related Links
- prostaglandin [pros″tah-glan´din] any of a group of naturally occurring, chemically related, long-chain hydroxy fatty acids that stimulate contractility of the uterine and other smooth muscle and have the ability to lower blood pressure ...
- 1. Dan Med J. 2013 May;60(5):B4635. Prostaglandins and prostaglandin receptor antagonism in migraine. Antonova M(1). Author information: (1)Department of Neurology, Danish Headache Center, Glostrup Hospital, Nordre ...
Related Pictures
★リンクテーブル★
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- 英
- prostaglandin antagonist
- 関
- プロスタグランジン阻害剤、プロスタグランジン受容体遮断薬
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- 英
- prostaglandin antagonist
- 関
- プロスタグランジン拮抗薬、プロスタグランジン阻害剤
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- 関
- prostaglandin antagonist
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プロスタグランジン prostaglandins PG
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プロスタグランジン