-
Eptapirone fumarate
- names:
4-Methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione fumarate
- CAS號:
179756-85-5
MDL Number: - MF(分子式): C20H27N7O6 MW(分子量): 461.479
- EINECS: Reaxys Number:
- Pubchem ID: Brand:BIOFOUNT
| 貨品編碼 | 規格 | 純度 | 價格 (¥) | 現價(¥) | 特價(¥) | 庫存描述 | 數量 | 總計 (¥) |
|---|
| 中文別名 | Eptapirone fumarate |
| 英文別名 | Eptapirone; F11440; F-11440; F 11440. |
| CAS號 | 179756-85-5 |
| Inchi | InChI=1S/C16H23N7O2.C4H4O4/c1-20-14(24)13-19-23(16(20)25)8-3-2-7-21-9-11-22(12-10-21)15-17-5-4-6-18-15;5-3(6)1-2-4(7)8/h4-6,13H,2-3,7-12H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+ |
| InchiKey | IRTCWPNSLGQHOR-WLHGVMLRSA-N |
| 分子式 Formula | C20H27N7O6 |
| 分子量 Molecular Weight | 461.479 |
| 溶解度Solubility | |
| 性狀 | Solid powder |
| 儲藏條件 Storage conditions | Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years). |
| 產品說明 | Eptapirone fumarate(CAS:179756-85-5 ):僅限應用于工業或者科學研究過程中非醫療目的,不應用于人類或動物的臨床診斷以及治過程療,該產品非藥用,非食用。 |
| Introduction | Eptapirone, also known as F11440, is a potent 5HT(1A) receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). |
| Application1 | |
| Application2 | |
| Application3 |
| [1]Koek W, Patoiseau JF, Assié MB, Cosi C, Kleven MS, Dupont-Passelaigue E, Carilla-Durand E, Palmier C, Valentin JP, John G, Pauwels PJ, Tarayre JP, Colpaert FC. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. J Pharmacol Exp Ther. 1998 Oct;287(1):266-83. PubMed PMID: 9765347. |
| [2]Thomas GH, Babbs AJ, Chatfield RE, Krülle TM, Widdowson PS, Provost D, McCormack JG. 5-HT(1A) activation counteracts cardiovascular but not hypophagic effects of sibutramine in rats. Obesity (Silver Spring). 2009 Mar;17(3):467-73. doi: 10.1038/oby.2008.550. PubMed PMID: 19219064. |
| [3] Wilson SJ, Bailey JE, Nutt DJ. Dizziness produced by a potent 5HT(1A) receptor agonist (eptapirone) is not due to postural hypotension. Psychopharmacology (Berl). 2005 Jun;179(4):895-6. PubMed PMID: 15619110. |
| [4] Wilson SJ, Bailey JE, Rich AS, Nash J, Adrover M, Tournoux A, Nutt DJ. The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J Psychopharmacol. 2005 Nov;19(6):609-13. PubMed PMID: 16272182. |
| [5] Pauwels PJ, Colpaert FC. Ca2+ responses in Chinese hamster ovary-K1 cells demonstrate an atypical pattern of ligand-induced 5-HT1A receptor activation. J Pharmacol Exp Ther. 2003 Nov;307(2):608-14. PubMed PMID: 12970382. |
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