1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. Pentiapine

Pentiapine (Synonyms: CGS 10746)

Cat. No.: HY-100143 Purity: 99.74%
Handling Instructions

Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites.

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

Pentiapine Chemical Structure

Pentiapine Chemical Structure

CAS No. : 81382-51-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 2473 In-stock
Estimated Time of Arrival: December 31
1 mg USD 751 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1202 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1923 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites[1][2].

IC50 & Target

Dopamine receptor[1]

In Vivo

Pentiapine is a novel dopamine release inhibitor.The results show that Pentiapine dose-dependently reduces motor activity of mice. Moreover, Pentiapine dose-dependently reduces morphine-induced hyperactivity. Newman-Keuls post-hoc comparisons indicate that the group receiving morphine plus saline presents more activity than the groups receiving morphine plus 2 (P<0.05), 4, 8, 16, 24 and 32 (P<0.01) mg/kg of Pentiapine. Moreover, the groups receiving morphine plus 0.5, 1 and 2 mg/kg of Pentiapine present more activity than the groups receiving morphine plus 4, 8, 16, 24 and 32 mg/kg of Pentiapine (P<0.01)[1]. 30 mg/kg dose of Pentiapine completely blocks the methylenedioxymethamphetamine (MDMA) conditioned place preference (CPP) and also blocks the establishment of a cocaine CPP[2].

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

Molecular Weight

299.39

Formula

C₁₅H₁₇N₅S

CAS No.

81382-51-6

SMILES

CN1CCN(C2=NC3=CC=CC=C3SC4=NC=CN42)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (334.01 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3401 mL 16.7006 mL 33.4012 mL
5 mM 0.6680 mL 3.3401 mL 6.6802 mL
10 mM 0.3340 mL 1.6701 mL 3.3401 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: ≥ 2.08 mg/mL (6.95 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.95 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (6.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Two hundred and fifty-seven male mice are used in this study. Animals are divided into 19 groups (n=8). The first group receives physiological saline, the second receives 40 mg/kg of morphine and the other eight groups receive 0.5, 1, 2, 4, 8, 16, 24 or 32 mg/kg of Pentiapine, respectively. The remaining groups receive an injection of morphine and 30 min afterwards, an injection of physiological saline, 0.5, 1, 2, 4, 8, 16, 24 or 32 mg/kg of Pentiapine, respectively. In the groups receiving only one injection, animals are placed onto the sensory plates for a period of 90 min immediately after treatment. The computer registers the activity each 15 min. In the groups receiving two injections, animals are placed onto the sensory plates immediately after the first injection for a period of 30 min then after the second injection the motor activity is registered at 15, 30, 45 and 60 min[1].

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

References

Purity: 99.74%

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Keywords:

PentiapineCGS 10746CGS10746CGS-10746Dopamine ReceptorInhibitorinhibitorinhibit

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