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4-methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3, 5-dione
For research use only. Not for therapeutic Use.
Eptapirone, also known as F11440, is a potent, selective, high efficacy 5-HT1A 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.
| Catalog Number | M044828 |
| CAS Number | 179756-85-5 |
| Synonyms | 4-methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3, 5-dione |
| Molecular Formula | C16H23N7O2 |
| Purity | ≥95% |
| Target | 5HT(1A) receptor agonist |
| Storage | -20°C |
| Reference | </br>1: Thomas GH, Babbs AJ, Chatfield RE, Krülle TM, Widdowson PS, Provost D,</br> McCormack JG. 5-HT(1A) activation counteracts cardiovascular but not hypophagic</br> effects of sibutramine in rats. Obesity (Silver Spring). 2009 Mar;17(3):467-73.</br> doi: 10.1038/oby.2008.550. Epub 2008 Dec 11. PubMed PMID: 19219064.</br>2: Wilson SJ, Bailey JE, Rich AS, Nash J, Adrover M, Tournoux A, Nutt DJ. The use</br> of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J</br> Psychopharmacol. 2005 Nov;19(6):609-13. PubMed PMID: 16272182.</br>3: Wilson SJ, Bailey JE, Nutt DJ. Dizziness produced by a potent 5HT(1A) receptor</br> agonist (eptapirone) is not due to postural hypotension. Psychopharmacology</br> (Berl). 2005 Jun;179(4):895-6. Epub 2004 Dec 24. PubMed PMID: 15619110.</br>4: Pauwels PJ, Colpaert FC. Ca2+ responses in Chinese hamster ovary-K1 cells</br> demonstrate an atypical pattern of ligand-induced 5-HT1A receptor activation. J</br> Pharmacol Exp Ther. 2003 Nov;307(2):608-14. Epub 2003 Sep 11. PubMed PMID:</br> 12970382.</br>5: Prinssen EP, Colpaert FC, Koek W. 5-HT1A receptor activation and</br> anti-cataleptic effects: high-efficacy agonists maximally inhibit</br> haloperidol-induced catalepsy. Eur J Pharmacol. 2002 Oct 25;453(2-3):217-21.</br> PubMed PMID: 12398907.</br>6: Koek W, Patoiseau JF, Assié MB, Cosi C, Kleven MS, Dupont-Passelaigue E,</br> Carilla-Durand E, Palmier C, Valentin JP, John G, Pauwels PJ, Tarayre JP,</br> Colpaert FC. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist </br> with marked anxiolytic and antidepressant potential. J Pharmacol Exp Ther. 1998</br> Oct;287(1):266-83. PubMed PMID: 9765347.</br></br> |
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