Pimozide-d4 (Synonyms: R6238-d4) |
| Katalog-Nr.GC45756 |
Pimozid D4 (R6238 D4) ist ein mit Deuterium gekennzeichnetes Pimozid.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1803193-57-8
Sample solution is provided at 25 µL, 10mM.
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Pimozide-d4 is an internal standard for the quantification of pimozide by GC- or LC-MS. Pimozide is a dopamine receptor antagonist (Kis = 2.4, 0.3, and 1.8 nM for D2, D3, and D4 receptors, respectively).1 It also binds to eight additional receptors (Kds = 25-3,100 nM for the human receptors) and inhibits the voltage-gated sodium channel Nav1.2 and the voltage-gated potassium channel Kv11.1 (IC50s = 42 and 340 nM, respectively).2,3,4 Pimozide (0.5, 1, and 2 mg/kg) decreases the number of licks and reduces fluid intake of a sweetened solution in rats.5 It decreases the number of threats and attacks and increases immobility time in the neutral arena aggression test, indicating increased passiveness, in male mice when administered at a dose of 0.75 mg/kg for 10 days.6 Formulations containing pimozide have been used in the treatment of Tourette syndrome.
|1. Burstein, E.S., Ma, J., Wong, S., et al. Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist. J. Pharmacol. Exp. Ther. 315(3), 1278-1287 (2005).|2. Richelson, E., and Souder, T. Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 68(1), 29-39 (2000).|3. Roufos, I., Hay, S., and Schwarz, R.D. A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers. J. Med. Chem. 39(7), 1514-1520 (1996).|4. Lau, J.F., Jeppesen, C.B., Rimvall, K., et al. Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides. Bioorg. Med. Chem. Lett. 16(20), 5303-5308 (2006).|5. Xenakis, S., and Sclafani, A. The effects of pimozide on the consumption of a palatable saccharin-glucose solution in the rat. Pharmacol. Biochem. Behav. 15(3), 435-442 (1980).|6. Navarro, J.F., Velasco, R., and Manzaneque, J.M. Acute and subchronic effects of pimozide on isolation-induced aggression in male mice. Prog. Neuropsychopharmacol. Biol. Psychiatry 24(1), 131-142 (2000).
| Cas No. | 1803193-57-8 | SDF | |
| Überlieferungen | R6238-d4 | ||
| Canonical SMILES | FC1=CC=C(C(CCCN2CCC(N3C(NC4=C3C=CC=C4)=O)CC2)C5=C([2H])C([2H])=C(F)C([2H])=C5[2H])C=C1 | ||
| Formula | C28H25D4F2N3O | M.Wt | 465.6 |
| Löslichkeit | Acetonitrile:Methanol (1:1): soluble | 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 | 2.1478 mL | 10.7388 mL | 21.4777 mL |
| 5 mM | 0.4296 mL | 2.1478 mL | 4.2955 mL |
| 10 mM | 0.2148 mL | 1.0739 mL | 2.1478 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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