Home Neuronal Signaling 5-HT Receptor antagonist - Dopamine Receptor antagonist Perospirone hydrochloride For research use only.

Perospirone hydrochloride

Synonyms: SM-9018 hydrochloride

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 Chemical Structure

Perospirone hydrochloride Chemical Structure

CAS No. 129273-38-7

Purity & Quality Control

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

Perospirone hydrochloride Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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 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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Five-week old male ICR mice
Dosages 10 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 463.04 Formula

C23H30N4O2S.HCl
CAS No. 129273-38-7 SDF --
Smiles C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (198.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 5 mg/mL


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In vivo
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