;関:15-hydroxy-11alpha
- 関
- 15-hydroxy-11alpha,9alpha-(epoxymethano)prosta-5,13-dienoic acid、U-46619
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/02/02 16:50:29」(JST)
[Wiki en表示]
| U46619 |
|
IUPAC name
(Z)-7-[(1S,4R,5R,6S)-5-[(E,3S)-3-hydroxyoct-1-enyl]-3-oxabicyclo[2.2.1]heptan-6-yl]hept-5-enoic acid
|
| Identifiers |
| CAS number |
56985-40-1 |
| PubChem |
5311493 |
| ChEMBL |
CHEMBL357834 |
| IUPHAR ligand |
1888 |
| Jmol-3D images |
Image 1 |
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CCCCC[C@H](O)/C=C/[C@H]1[C@@H]2OC[C@@H](C2)[C@@H]1C/C=C\CCCC(O)=O
|
| Properties |
| Molecular formula |
C21H34O4 |
| Molar mass |
350.49 g/mol |
| Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa) |
| Y (verify) (what is: Y/N?) |
| Infobox references |
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U46619 is a stable synthetic analog of the endoperoxide prostaglandin PGH2 first prepared in 1975,[1] and acts as a thromboxane A2 (TP) receptor agonist.[2] It potently stimulates TP receptor-mediated, but not other prostaglandin receptor-mediated responses in various in vitro preparations.[3] and exhibits many properties similar to thromboxane A2, including shape change and aggregation of platelets [4] and smooth muscle contraction. U46619 is a vasoconstrictor that mimics the hydroosmotic effect of vasopressin.[5]
References
- ^ Bundy, G. L. (1975). "Synthesis of prostaglandin endoperoxide analogs". Tetrahedron Letters 24 (24): 1957–1960. doi:10.1016/S0040-4039(00)72333-1.
- ^ "U 46619". www.tocris.com.
- ^ "U 46619". www.tocris.com.
- ^ Liel, N.; Mais, D.E.; Halushka, P.V (1987). "Binding of a thromboxane A2/prostaglandin H2 agonist [3H]U46619 to washed human platelets". Prostaglandins 33: 789–797. doi:10.1016/0090-6980(87)90107-9.
- ^ Burch, Ronald M.; Halushka, Perry V. (1983). "Calcium-45 fluxes in isolated toad bladder epithelial cells: effects of agents which alter water or sodium transport". Journal of Pharmacology and Experimental Therapeutics 224 (1): 108–17. PMID 6294273.
UpToDate Contents
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English Journal
- Contribution of BKCa channels to vascular tone regulation by PDE3 and PDE4 is lost in heart failure.
- Idres S1, Perrin G1, Domergue V2, Lefebvre F1, Gomez S1, Varin A1, Fischmeister R1, Leblais V1, Manoury B1.
- Cardiovascular research.Cardiovasc Res.2019 Jan 1;115(1):130-144. doi: 10.1093/cvr/cvy161.
- PMID 29939224
- Systemic microvascular dysfunction in microvascular and vasospastic angina.
- Ford TJ1,2,3, Rocchiccioli P1,2, Good R1, McEntegart M1,2, Eteiba H1, Watkins S1, Shaukat A1, Lindsay M1, Robertson K1, Hood S1, Yii E2, Sidik N2, Harvey A2, Montezano AC2, Beattie E2, Haddow L2, Oldroyd KG1, Touyz RM2, Berry C1,2.
- European heart journal.Eur Heart J.2018 Dec 7;39(46):4086-4097. doi: 10.1093/eurheartj/ehy529.
- PMID 30165438
- Platelet dysfunction during trauma involves diverse signaling pathways and an inhibitory activity in patient-derived plasma.
- Verni CC1, Davila A Jr2, Balian S2, Sims CA2,3, Diamond SL.
- The journal of trauma and acute care surgery.J Trauma Acute Care Surg.2018 Dec 6. doi: 10.1097/TA.0000000000002140. [Epub ahead of print]
- PMID 30531331
Japanese Journal
- Thromboxane A2 Mediates Iron-Overload Cardiomyopathy in Mice Through Calcineurin-Nuclear Factor of Activated T Cells Signaling Pathway
- Lin Heng,Li Hsiao-Fen,Lian Wei-Shiung,Chen Hsi-Hsien,Lan Yi-Fan,Lai Pei-Fang,Cheng Ching-Feng
- Circulation Journal, 2013
- … Using a TXA2 analog, U46619, for NFAT reporter luciferase activity on cardiomyoctes, and intraperitonal injection of U46619 into nuclear factor of activated T cells (NFAT)-luciferase transgenic mice demonstrated that U46619 increase NFAT expression, and this expression, as well as TNF-α expression, can be blocked by TXA2 receptor antagonist (SQ29548), NFAT-SiRNA, calcineurin inhibitor, or calcium chelator. …
- NAID 130003361810
- P-02 U46619による血管張力制御機構の検討(ポスターセッション1,一般演題(ポスター),第54回日本平滑筋学会総会)
- 高野 博充,Dora Kim A,Garland Christopher J,橋谷 光
- 日本平滑筋学会雑誌 16(1), "J-41", 2012-07-02
- NAID 110009479589
- Acute Modulation of Vasoconstrictor Responses by Pravastatin in Small Vessels
- GHAFFARI Nader,BALL Christine,KENNEDY Jennifer A,STAFFORD Irene,BELTRAME John F
- Circulation journal : official journal of the Japanese Circulation Society 75(6), 1506-1514, 2011-05-25
- … Methods and Results: Pravastatin (112nmol/L) pretreatment for 60min reduced both the potency and maximal constrictor responses to phenylephrine, thromboxane (U46619) and serotonin in small vessels. …
- NAID 10028149391
★リンクテーブル★
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15-ヒドロキシ-11α
- 関
- U-46619、U46619