A 5-HT2, 5-HT1A, and dopamine D2 receptor antagonist
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Perospirone

Item No. 46279

Technical Information
Formal Name
(3aR,7aS)-rel-2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-1H-isoindole-1,3(2H)-dione
CAS Number
150915-41-6
Synonyms
  • SM-9018
Molecular Formula
C23H30N4O2S
Formula Weight
Purity
≥98%
A solid
SMILES
[H][C@@]1(C2=O)CCCC[C@](C(N2CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54)=O)1[H]
InChi Code
InChI=1S/C23H30N4O2S/c28-22-17-7-1-2-8-18(17)23(29)27(22)12-6-5-11-25-13-15-26(16-14-25)21-19-9-3-4-10-20(19)30-24-21/h3-4,9-10,17-18H,1-2,5-8,11-16H2/t17-,18+
InChi Key
FBVFZWUMDDXLLG-HDICACEKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Perospirone is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2 and 5-HT1A and the dopamine D2 receptor (Kis = 0.61, 2.9, and 1.4 nM, respectively, in rat brain membranes).1 It is selective for these receptors over the dopamine D1 and α1- and α2-adrenergic receptors (Kis = 41, 17, and 408 nM, respectively) and a panel of six other receptors (Kis = >1,000 nM for all). Perospirone inhibits clonic seizures induced by tryptamine (Item No. 20995) and reduces hyperactivity induced by methamphetamine in rats and climbing behavior induced by apomorphine in mice (ED50s = 1.4, 2.2, and 3.5 mg/kg, respectively) but does not induce catalepsy in rats or mice.2 Formulations containing perospirone have been used in the treatment of schizophrenia and acute bipolar mania.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kato, T., Hirose, A., Ohno, Y., et al. Binding profile of SM-9018, a novel antipsychotic candidate. Jpn. J. Pharmacol. 54(4), 478-481 (1990).

    2. Hirose, A., Kato, T., Ohno, Y., et al. Pharmacological actions of SM-9018, a new neuroleptic drug with both potent 5-hydroxytryptamine2 and dopamine2 antagonistic actions. Jpn. J. Pharmacol. 53(3), 321-329 (1990).