Perospirone hydrochloride

Catalog No.S4889 Batch:S488901

Technical Data

Formula	C₂₃H₃₀N₄O₂S.HCl
Molecular Weight	463.04	CAS No.	129273-38-7
Solubility (25°C)*	In vitro	DMSO	92 mg/mL (198.68 mM)
		Water	5 mg/mL (10.79 mM)

* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Perospirone (SM-9018) 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 (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[4]}	Animal Models Five-week old male ICR mice Dosages 10 mg/kg Administration p.o.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[4]}

Animal Models
Five-week old male ICR mice
Dosages
10 mg/kg
Administration
p.o.

References

[4] Matsushita M, et al. J Pharmacol Sci. 2005, 99(2):154-9.

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Selleck's Perospirone hydrochloride has been cited by 1 publication

NFX1-123: A potential therapeutic target in cervical cancer [ J Med Virol, 2023, 95(6):e28856]	PubMed: 37288708

NFX1-123: A potential therapeutic target in cervical cancer [ J Med Virol, 2023, 95(6):e28856]

PubMed: 37288708

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SHIPPING AND STORAGE
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