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Perospirone

Catalog No. T4576 CAS 150915-41-6

Synonyms: Lullan

Perospirone (Lullan) is an antagonist of serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

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Perospirone, CAS 150915-41-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 101.00
25 mg	In stock	$ 190.00
50 mg	In stock	$ 343.00
100 mg	In stock	$ 587.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 98.86%

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Description	Perospirone (Lullan) is an antagonist of serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.
Targets&IC50	5-HT1A:2.9 nM (Ki), D2:0.6 nM (Ki), 5-HT2A:1.3 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 behaviours (e.g. methamphetamine-induced hyperactivity and apomorphine-induced stereotypy or climbing behaviour) in rodents. It also inhibits the rat conditioned avoidance response. In behavioural tests, perospirone markedly inhibits serotonergic behaviour (e.g. tryptamine-induced clonic seizures, and p-chlorphenamine-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 anaesthesia with ED50 values of 34 and 37 mg/kg (p.o.), respectively[1].
Cell Research	Cell lines: Human neuroblastoma SK-N-SH cells. Concentrations: 10.5 or 105.5?nM.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 Research	Animal Models: Five-week-old male ICR mice. Formulation: 0.5% methylcellulose solution. Dosages: 10 mg/kg, p.o.

Synonyms	Lullan
Molecular Weight	426.57
Formula	C23H30N4O2S
CAS No.	150915-41-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (128.94 mM)

References and Literature

1. Ishibashi T, Ohno Y. Perospirone hydrochloride: the novel atypical antipsychotic agent with high affinities for 5-HT2, D2 and 5-HT1A receptors[J]. Biogenic Amines, 2004, 18(3):307-317. 2. Murata Y, et al. DNA Methylation Profiling in a Neuroblastoma Cell Line Exposed to the Antipsychotic Perospirone[J]. Pharmacopsychiatry, 2018. 3. Zhou Y G, et al. Effect of the novel antipsychotic drug perospirone on P-glycoprotein function and expression in Caco-2 cells[J]. European Journal of Clinical Pharmacology, 2008, 64(7):697-703. 4. Matsushita M, et al. Perospirone, a novel antipsychotic drug, inhibits marble-burying behavior via 5-HT1A receptor in mice: implications for obsessive-compulsive disorder.[J]. Journal of Pharmacological Sciences, 2005, 99(2):154-159.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Drug Library Anti-Parkinson's Disease Compound Library Anti-Hypertension Compound Library Orally Active Compound Library Anti-Alzheimer's Disease Compound Library

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Keywords

Perospirone 150915-41-6 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor deficits atypical SM-9018 5-hydroxytryptamine Receptor Orally SM9018 schizophrenic disease Serotonin Receptor cognitive Inhibitor SM 9018 inhibit antipsychotic Lullan inhibitor

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