A potent and selective 5-HT1A receptor agonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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 (Request formulation change)
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $41

    Add

    5 mg

    $178

    Add

    10 mg

    $332

    Add

    25 mg

    $680

    Add
    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).