Home Neuronal Signaling 5-HT Receptor antagonist - Dopamine Receptor antagonist Perospirone hydrochloride

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Perospirone hydrochloride 5-HT Receptor antagonist

Cat.No.S4889

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.
Perospirone hydrochloride 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 463.04

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Quality Control

Batch: S488901 DMSO]92 mg/mL]false]Water]5 mg/mL]false]]]false Purity: 98%
98

Chemical Information, Storage & Stability

Molecular Weight 463.04 Formula

C23H30N4O2S.HCl

 Storage (From the date of receipt)
CAS No. 129273-38-7 -- Storage of Stock Solutions

Synonyms SM-9018 hydrochloride Smiles C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54.Cl

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (198.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 5 mg/mL

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
5-HT2 receptor [1]
(in rat brain membrane preparation)
0.61 nM(Ki)
D2 receptor [1]
(in rat brain membrane preparation)
1.4 nM(Ki)
5HT1A receptor [1]
(in rat hippocampal membrane preparation)
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].
References

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