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M6595-2 2mg solid $124
M6595-10 10mg solid $476


Eptapirone, also known as F11440 and L0068, 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.

Product information

CAS Number: 179756-58-2

Molecular Weight: 345.40

Formula: C16H23N7O2




Eptapirone free base


F 11440



L 0068

Chemical Name: 4-Methyl-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-as-triazine-3,5(2H,4H)-dione



InChi: InChI=1S/C16H23N7O2/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/h4-6,13H,2-3,7-12H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

The affinity of Eptapirone (F11440) for 5-HT1Abinding 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, Eptapirone (F11440) 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). Eptapirone (F11440), shown here to be a potent, selective, high efficacy 5-HT1Areceptor agonist, appears to have the potential to exert marked anxiolytic and antidepressant activity in humans.


  1. 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.
  2. 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. Epub 2004 Dec 24. PubMed PMID: 15619110.
  3. 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. Epub 2003 Sep 11. PubMed PMID: 12970382.
  4. Prinssen EP, Colpaert FC, Koek W. 5-HT1A receptor activation andanti-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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