179756-85-5|Eptapirone fumarate|4-Methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione fumarate|-范德生物科技公司

Eptapirone fumarate

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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

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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
SMILES	O=C(N1C)N(CCCCN2CCN(C3=NC=CC=N3)CC2)N=CC1=O.O=C(O)/C=C/C(O)=O
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
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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。
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
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危险性	Warning
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安全声明
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备注

[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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