Home Neuronal Signaling 5-HT 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

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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In vivo
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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

Mechanism of Action

Targets/IC50/Ki
5-HT2 receptor
(in rat brain membrane preparation)
0.61 nM(Ki)
D2 receptor
(in rat brain membrane preparation)
1.4 nM(Ki)
5HT1A receptor
(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. 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.
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16210777/

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