Pentiapine (CGS 10746) |
| カタログ番号GC33730 |
ペンティアピン (CGS 10746) (CGS 10746) は、シナプス ドーパミン受容体部位に結合しないドーパミン放出阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 81382-51-6
Sample solution is provided at 25 µL, 10mM.
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Pentiapine is a novel dopamine release inhibitor.
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].
[1]. Manzanedo C, et al. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32. [2]. Bilsky EJ, et al. CGS 10746B, a novel dopamine release inhibitor, blocks the establishment of cocaine and MDMA conditioned place preferences. Pharmacol Biochem Behav. 1998 Jan;59(1):215-20.
Animal experiment: | 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]. |
References: [1]. Manzanedo C, et al. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32. | |
| Cas No. | 81382-51-6 | SDF | |
| Canonical SMILES | CN1CCN(C2=NC3=CC=CC=C3SC4=NC=CN42)CC1 | ||
| Formula | C15H17N5S | M.Wt | 299.39 |
| 溶解度 | DMSO: 100 mg/mL (334.01 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3401 mL | 16.7006 mL | 33.4012 mL |
| 5 mM | 668 μL | 3.3401 mL | 6.6802 mL |
| 10 mM | 334 μL | 1.6701 mL | 3.3401 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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