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179756-85-5
  • Eptapirone fumarate

  • names:

    4-Methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione fumarate

  • CAS号:

    179756-85-5

    MDL Number:
  • MF(分子式): C20H27N7O6 MW(分子量): 461.479
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Eptapirone fumarate
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中文别名 Eptapirone fumarate
英文别名 Eptapirone; F11440; F-11440; F 11440.
CAS号 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
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 Eptapirone fumarate(CAS:179756-85-5 ):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionEptapirone, 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).
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[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.
6: Prinssen EP, Colpaert FC, Koek W. 5-HT1A receptor activation and anti-cataleptic effects: high-efficacy agonists maximally inhibit haloperidol-induced catalepsy. Eur J Pharmacol. 2002 Oct 25;453(2-3):217-21. PubMed PMID: 12398907.
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