A potent and selective 5-HT1A receptor agonist
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Eptapirone

Item No. 23449

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-methyl-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,2,4-triazine-3,5(2H,4H)-dione
CAS Number
179756-58-2
Synonyms
  • F 11440
Molecular Formula
C16H23N7O2
Formula Weight
345.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:40): 0.025 mg/mlEthanol: slightly soluble
λmax
204, 243 nm
SMILES
O=C(C=N1)N(C)C(N1CCCCN(CC2)CCN2C3=NC=CC=N3)=O
InChi Code
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
InChi Key
NMYAHEULKSYAPP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).1 It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = <10,000, 1,770, 691.8, and <10,000 nM, respectively). Eptapirone inhibits cAMP stimulation induced by forskolin (Item No. 11018) in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT (Item No. 14332) in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone (Item No. 16063) levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine (Item No. 14476) in rats with no effect on sibutramine-induced hypophagia.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Koek, W., Patoiseau, J.-F., Assie, M.-B., et al. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. J.Pharmacol. Exp. Ther. 287(1), 266-283 (1998).

    2. Thomas, G.H., Babbs, A.J., Chatfield, R.E., et al. 5-HT1A activation counteracts cardiovascular but not hypophagic effects of sibutramine in rats. Obesity (Silver Spring) 17(3), 467-473 (2009).