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 2 publications

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
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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