Perospirone hydrochloride

Catalog No.S4889 Synonyms: SM-9018 hydrochloride

Perospirone hydrochloride Chemical Structure

Molecular Weight(MW): 463.04

Perospirone is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

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Biological Activity

Description Perospirone is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.
Targets
5-HT2 receptor [1]
(in rat brain membrane preparation)
D2 receptor [1]
(in rat brain membrane preparation)
5HT1A receptor [1]
(in rat hippocampal membrane preparation)
0.61 nM(Ki) 1.4 nM(Ki) 2.9 nM(Ki)
In vitro

In CHO cells expressing human 5-HT1A receptors, perospirone shows a high affinity (Ki = 0.72 nM), and exhibits partial agonistic efficacy[1]. Perospirone changes epigenetic profiles of neural genes. It can cause DNA methylation changes in cell cultures[2]. Perospirone is an inhibitor of Pgp which interferes directly and indirectly with the function of Pgp. The inhibition of Pgp by perospirone may cause clinically significant drug-drug interactions, especially in the tissue in which it accumulated[3].

In vivo Perospirone shows potent 5-HT2 and D2 receptor blocking activities in various animal models in vivo. Perospirone inhibits various dopaminergic behaviors (e.g. methamphetamine-induced hyperactivity and apomorphine-induced stereotypy or climbing behavior) in rodents. It also inhibits the rat conditioned avoidance response. In behavioral tests, perospirone markedly inhibits serotonergic behavior (e.g. tryptamine-induced clonic seizures, and p-chloramphetamine-induced hyperthermia) in rats. Perospirone has anxiolytic-like effects and mood stabilizing effects in various animal models. It inhibits motor coordination in a rota-rod test, and potentiates the duration of hexobarbital-induced anesthesia with ED50 values of 34 and 37 mg/kg (p.o.), respectively[1].

Protocol

Cell Research:[2]
+ Expand
  • Cell lines: Human neuroblastoma SK-N-SH cells
  • Concentrations: 10.5 nM and 105.5 nM
  • Incubation Time: 9 days
  • Method: cells are maintained in Eagle's minimal essential medium containing 10% fetal bovine serum for 8 days. The cells are exposed to either a high dose (105.5 nM, assigned as the "high-dose group") or low dose (10.5 nM, assigned as the "low-dose group") of perospirone. The concentrations are determined based on dosages typically used in the clinical setting. The medium is changed on days 2, 5, and 8 with media containing perospirone, and on day 9, cells are harvested and processed.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Five-week old male ICR mice
  • Formulation: 0.5% methylcellulose solution
  • Dosages: 10 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (198.68 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 463.04
Formula

C23H30N4O2S.HCl

CAS No. 129273-38-7
Storage powder
in solvent
Synonyms SM-9018 hydrochloride

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID