A 5-HT1A receptor partial agonist
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Active Metabolite(s)
340912-(1-Piperazinyl)pyrimidine
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Gepirone

Item No. 46176

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione
CAS Number
83928-76-1
Synonyms
  • BMY 13805
  • MJ13805
  • Org 13011
Molecular Formula
C19H29N5O2
Formula Weight
359.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/mlPBS (pH 7.2): Sparingly soluble: 1-10 mg/ml
SMILES
O=C1N(CCCCN2CCN(CC2)C3=NC=CC=N3)C(CC(C)(C1)C)=O
InChi Code
InChI=1S/C19H29N5O2/c1-19(2)14-16(25)24(17(26)15-19)9-4-3-8-22-10-12-23(13-11-22)18-20-6-5-7-21-18/h5-7H,3-4,8-15H2,1-2H3
InChi Key
QOIGKGMMAGJZNZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $55

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    10 mg

    $105

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    50 mg

    $220

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    100 mg

    $330

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    Product Description

    Gepirone is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A.1,2,3 It binds to the 5-HT1A receptor with a Ki value of 31.8 nM.1 Gepirone (5 mg/kg) reduces 5-HT release in rat ventral hippocampus in vivo.4 It decreases depressive-like, aggressive, and anxiety-like behavior in mice.2,3 Gepirone also prevents clonidine-induced slowing of gastrointestinal transit in rats (ED50 = 9.3 mg/kg).5 Formulations containing gepirone have been used in the treatment of major depressive disorder (MDD).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mokrosz, J.L., Pietrasiewicz, M., Duszyńska, B., et al. Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site. J. Med. Chem. 35(13), 2369-2374 (2002).

    2. Wieland, S., and Lucki, I. Antidepressant-like activity of 5-HT1A agonists measured with the forced swim test. Psychopharmacology (Berl.) 101(4), 497-504 (1990).

    3. Mendoza, D.L., Bravo, H.A., and Swanson, H.H. Antiaggresive and anxiolytic effects of gepirone in mice, and their attenuation by WAY 100635. Pharmacol. Biochem. Behav. 62(3), 499-509 (1999).

    4. Sharp, T., Bramwell, S.R., and Grahame-Smith, D.G. 5-HT1 agonists reduce 5-hydroxytryptamine release in rat hippocampus in vivo as determined by brain microdialysis. Br. J. Pharmacol. 96(2), 283-290 (1989).

    5. Bianchi, G., Caccia, S., Della Vedova, F., et al. The α2-adrenoceptor antagonist activity of ipsapirone and gepirone is mediated by their common metabolite 1-(2-pyrimidinyl)-piperazine (PmP). Eur. J. Pharmacol. 151(3), 365-371 (1988).