A dopamine D2 and D3 receptor antagonist
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Fluspirilene

Item No. 19530

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
CAS Number
1841-19-6
Synonyms
  • McN-JR 6218
  • R 6218
  • Redeptin
Molecular Formula
C29H31F2N3O
Formula Weight
475.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 10 mg/mlEthanol: 0.3 mg/ml
λmax
252, 272, 293 nm
SMILES
FC1=CC=C(C(C2=CC=C(F)C=C2)CCCN3CCC4(C(NCN4C5=CC=CC=C5)=O)CC3)C=C1
InChi Code
InChI=1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35)
InChi Key
QOYHHIBFXOOADH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $80

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    10 mg

    $141

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    25 mg

    $255

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    Product Description

    Fluspirilene is a dopamine D2 and D3 receptor antagonist (Kis = 1.5 and 1.1 nM, respectively).1 It is selective for dopamine D2 and D3 receptors over dopamine D1, α1- and α2-adrenergic, H1 histamine, and sigma-1 (σ1) receptors (Kis = 450, 102, >5,000, 540, and 150 nM, respectively), muscarinic acetylcholine receptors (mAChRs; Ki = >5,000 nM), and the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, 5-HT2C, and 5-HT3 (Kis = 110, >5,000, 1,830, and >5,000 nM, respectively). Fluspirilene is also a noncompetitive inhibitor of L-type calcium (Cav1) channels with an IC50 value of 30 nM.2 It inhibits apomorphine-induced vomiting in dogs (ED50 = 0.011 mg/kg).3 Formulations containing fluspirilene have been used in the treatment of schizophrenia.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schotte, A., Janssen, P.F., Gommeren, W., et al. Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor binding. Psychopharmacology (Berl) 124(1-2), 57-73 (1996).

    2. Kenny, B.A., Fraser, S., Kilpatrick, A.T., et al. Selective antagonism of calcium channel activators by fluspirilene. Br. J. Pharmacol. 100(2), 211-216 (1990).

    3. Janssen, P.A.J., Niemegeers, C.J.E., Schellekens, K.H.L., et al. Pharmacology of fluspirilene (R 6218) [8-[4,4-bis(p-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one] a potent, long-acting, and injectable neuroleptic drug. Arzneimittelforschung 20(11), 1689-1698.