1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor 5-HT Receptor
  3. Abaperidone

Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.

For research use only. We do not sell to patients.

Abaperidone Chemical Structure

Abaperidone Chemical Structure

CAS No. : 183849-43-6

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Description

Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.

IC50 & Target

D2 Receptor

17 nM (IC50)

5-HT2A Receptor

6.2 nM (IC50)

In Vitro

Abaperidone possesses good affinity for dopamine D2 receptors, together with a greater affinity for 5-HT2 receptors with IC50 of 17 and 6.2 nM, reaspectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The time course of the inhibition of climbing behavior for a period of several hours after oral administration of either 0.5 mg/kg of Abaperidone or risperidone is tested in mice. Also is included a comparative test of catalepsy induced by Abaperidone and risperidone along several hours following oral administration at several doses in rats. A somewhat lesser induction of catalepsy is observed for Abaperidone. A study of serum prolactin levels after oral administration of Abaperidone, haloperidol, and risperidone at 5 mg/kg for either 1 or 3 days in rats. Increases in prolactin levels after oral administration of Abaperidone are smaller than those for reference drugs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

452.47

Formula

C25H25FN2O5

CAS No.
SMILES

O=C1C(CO)=COC2=CC(OCCCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)=CC=C12

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
Kinase Assay
[1]

Receptor binding assays are performed by inhibition of radioligand binding according to reported procedures for D1, D2, D3, D4, 15a5-HT1A, 5-HT2A, α1, α2, β, muscarinic, and σ receptors. IC50 values are calculated from concentration−response curves at 11 different concentrations of the test compound, each done in duplicate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats[1]
Sprague-Dawley rats (220-240 g) are assigned to 8 groups of 5 animals each, and are orally dosed with either Abaperidone (5 mg/kg/day), Haloperidol (5 mg/kg/day), Risperidone (5 mg/kg/day), or the vehicle for 1 or 3 consecutive days. The animals are killed by decapitation 3 h after last dosing, blood samples of 2 mL are collected, and prolactin levels are determined by means of an EIA kit from Amersham.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
Abaperidone
Cat. No.:
HY-101619
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