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

Quetiapine (Synonyms: ICI204636)

Cat. No.: HY-14544 Purity: 99.96%
Handling Instructions

Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

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

Quetiapine Chemical Structure

Quetiapine Chemical Structure

CAS No. : 111974-69-7

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Based on 1 publication(s) in Google Scholar

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Description

Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].

IC50 & Target[1]

5-HT1A Receptor

5.74 (pKi)

5-HT2A Receptor

7.54 (pKi)

5-HT2C Receptor

5.55 (pKi)

D2 Receptor

7.25 (pKi)

5-HT1A Receptor

4.77 (pEC50)

D2 Receptor

6.33 (pIC50)

In Vitro

Quetiapine (ICI204636) is indicated for the treatment of schizophrenia as well as for the treatment of acute manic episodes associated with bipolar I disorder. The antipsychotic effect of quetiapine is thought by some to be mediated through antagonist activity at dopamine and serotonin receptors. Specifically the D1 and D2 dopamine, the alpha 1 adrenoreceptor and alpha 2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine (ICI204636) also has an antagonistic effect on the histamine H1 receptor.

Clinical Trial
Molecular Weight

383.51

Formula

C₂₁H₂₅N₃O₂S

CAS No.

111974-69-7

SMILES

OCCOCCN(CC1)CCN1C2=NC3=CC=CC=C3SC4=C2C=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (260.75 mM; Need ultrasonic)

DMSO : 100 mg/mL (260.75 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6075 mL 13.0375 mL 26.0749 mL
5 mM 0.5215 mL 2.6075 mL 5.2150 mL
10 mM 0.2607 mL 1.3037 mL 2.6075 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

QuetiapineICI204636ICI 204636ICI-2046365-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1AD25-HT2A5-HT2CAntidepressantanxiolyticInhibitorinhibitorinhibit

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Quetiapine
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