A selective D4 receptor antagonist
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Sonepiprazole

Item No. 11983

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[2-[(1S)-3,4-dihydro-1H-2-benzopyran-1-yl]ethyl]-1-piperazinyl]-benzenesulfonamide
CAS Number
170858-33-0
Synonyms
  • PNU 101387
  • U-101387
Molecular Formula
C21H27N3O3S
Formula Weight
401.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 0.2 mg/ml
λmax
265 nm
SMILES
O=S(C(C=C1)=CC=C1N(CC2)CCN2CC[C@H]3C(C=CC=C4)=C4CCO3)(N)=O
InChi Code
InChI=1S/C21H27N3O3S/c22-28(25,26)19-7-5-18(6-8-19)24-14-12-23(13-15-24)11-9-21-20-4-2-1-3-17(20)10-16-27-21/h1-8,21H,9-16H2,(H2,22,25,26)/t21-/m0/s1
InChi Key
WNUQCGWXPNGORO-NRFANRHFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

    $120

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    10 mg

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    Product Description

    Sonepiprazole is a selective antagonist of the dopamine 4 (D4) receptor (Kis = 10 nM). It is highly selective over D1, D2, and D3 receptors, serotonin 1A and 2 receptors, as well as α1- and α2-adrenergic receptors (Kis > 2,000 nM).1,2 Its safety profile in rat studies is improved in comparison to classical antipsychotics but it is not effective for positive or negative symptoms of schizophrenia in patients.1,3 In a pharmacological model of stress exposure in rhesus monkeys, sonepiprazole reverses stress-induced cognitive deficits.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Merchant, K.M., Gill, G.S., Harris, D.W., et al. Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. J. Pharmacol. Exp. Ther. 279(3), 1392-1403 (1996).

    2. Tenbrink, R.E., Bergh, C.L., Duncah, J.N., et al. (S)-(−)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. J. Med. Chem. 39(13), 2435-2437 (1996).

    3. Corrigan, M.H., Gallen, C.C., Bonura, M.L., et al. Effectiveness of the selective D4 antagonist sonepiprazole in schizophrenia: A placebo-controlled trial. Biol. Psychiatry 55(5), 445-451 (2004).

    4. Arnsten, A.F.T., Murphy, B., and Merchant, K. The selective dopamine D4 receptor antagonist, PNU-101387G, prevents stress-induced cognitive deficits in monkeys. Neuropsychopharmacology 23(4), 405-410 (2000).