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

Iloperidone hydrochloride (Synonyms: HP 873 hydrochloride)

Cat. No.: HY-17410A
Handling Instructions

Iloperidone hydrochloride (HP 873 hydrochloride) is a D2/5-HT2 receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms.

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

Iloperidone hydrochloride Chemical Structure

Iloperidone hydrochloride Chemical Structure

CAS No. : 1299470-39-5

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Description

Iloperidone hydrochloride (HP 873 hydrochloride) is a D2/5-HT2 receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms[1][2].

IC50 & Target[1]

Rat D2 Receptor

54 nM (Ki)

Rat 5-HT2 Receptor

3.1 nM (Ki)

Rat D1 Receptor

546 nM (Ki)

Rat 5-HT1A Receptor

168 nM (Ki)

Rat 5-HT6 Receptor

42.7 nM (Ki)

Rat 5-HT7 Receptor

21.6 nM (Ki)

Human D1 Receptor

216 nM (Ki)

Human D3 Receptor

7.1 nM (Ki)

Human D4 Receptor

25 nM (Ki)

Human D5 Receptor

319 nM (Ki)

Human 5-HT2A Receptor

5.6 nM (Ki)

Human 5-HT2C Receptor

42.8 nM (Ki)

In Vitro

Iloperidone hydrochloride displays higher affinity for the dopamine D3 receptor (Ki=7.1 nM) than for the dopamine D4 receptor (Ki=25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki=5.6 nM) than for the 5-HT2C receptor (Ki=42.8 nM)[1].

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

In Vivo

Iloperidone hydrochloride is eliminated slowly, with a mean t1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, tmax, or Cmax. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events[2].

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

Clinical Trial
Molecular Weight

462.94

Formula

C₂₄H₂₈ClFN₂O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Product Name:
Iloperidone hydrochloride
Cat. No.:
HY-17410A
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