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Perospirone

SKU: orb1302743

Description

Perospirone (Lullan) is an atypical antipsychotic agent functioning as a 5HT2A and D2 receptor antagonist with partial agonism at 5HT1A receptors. It is utilized in neuroscience research for investigating receptor interactions and pharmacological profiles in both in vitro binding assays and in vivo behavioral studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Perospirone

Key Properties

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CAS Number150915-41-6
MW426.57
Purity99.45% (May vary between batches)
FormulaC23H30N4O2S
SMILES[H][C@@]12CCCC[C@]1([H])C(=O)N(CCCCN1CCN(CC1)c1nsc3ccccc13)C2=O
Target5-HT Receptor|||Dopamine Receptor
SolubilityDMSO:55 mg/mL (128.94 mM)

Bioactivity

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Target IC50
D1 receptor:41 nM (Ki)|5-HT2A:1.3 nM (Ki)|D2:0.6 nM (Ki)|5-HT1A:2.9 nM (Ki)|5-HT1 receptor:18 nM (Ki)
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.
In Vitro
In CHO cells expressing human 5-HT1A receptors, perospirone shows a high affinity (Ki: 0.72 nM) and exhibits partial agonistic efficacy. Perospirone changes epigenetic profiles of neural genes. It can cause DNA methylation changes in cell cultures. 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.
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.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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D2, DopamineReceptor, Dopamine Receptor, Dopamine, disease, deficits, cognitive, atypical, antipsychotic, 5HTReceptor, 5-hydroxytryptamine Receptor, 5-HT Receptor, 5HT Receptor, 5-HT2A, 5-HT1A, Inhibitor, inhibit, Orally, Lullan, schizophrenic, SM 9018, SM9018, SM-9018, Serotonin Receptor, Perospirone

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Quality Guarantee

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
115368 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 ml x 10 mM (in DMSO)
$ 80.00
5 mg
$ 80.00
10 mg
$ 110.00
25 mg
$ 160.00
50 mg
$ 250.00
100 mg
$ 400.00
200 mg
$ 540.00
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