Loxapine |
| Katalog-Nr.GC13081 |
Loxapin ist ein oral aktiver Dopaminhemmer, 5-HT-Rezeptorantagonist und auch ein Dibenzoxazepin-Antipsychotikum.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1977/10/2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent [1].
In vitro: Loxapine was a typical neuroleptic that showed great structural and functional homology to the atypical antipsychotic clozapine. Chronic loxapine treatment was usually associated with extrapyramidal symptoms (EPS). Loxapineexihibited an extremely strong binding affinity fordopamineD4 andserotonin5-HT2receptors, suggesting that both serotonergic and dopaminergic mechanisms contributed to the antipsychotic drug action and EPS associated with loxapine in the treatment of schizophrenia [1]. In frontal cortex of brain in human and bovine, in the presence of Loxapine, [3H]ketanserin bound to 5-HT2 receptor with ki value of 6.2 nM and 6.6 nM, respectively. In comparing competition experiments involving the human membranes, loxapine exihibited the rank order of potency for the various receptors as follows: 5-HT2≥D4>>>D1>D2 [1]. Loxapine administration at 0.2, 2 and 20 μMafter 1 and 3 days of exposure reduced IL-1βand IL-2 secretion by LPS-activated mixed glia cultures. Loxapine also decreased IL-1βand IL-2 secretion in LPS-induced microglia cultures [2].
In vivo: Chronic administration of loxapine(5 mg/kg) in rats for 4 weeks or 10 weeks significantly reduced more than 50% of serotonin (S2) receptor density. Loxapine (5 mg/kg) didn’t change dopamine receptor density but greatly reduced serotonin receptor density by 47% in the brain of rats [3].
References:
[1]. Singh AN1,Barlas C,Singh S,Franks P,Mishra RK. A neurochemical basis for the antipsychotic activity of loxapine: interactions withdopamineD1,D2, D4 andserotonin5-HT2receptorsubtypes.J Psychiatry Neurosci.1996 Jan;21(1):29-35.
[2]. Labuzek K1,Kowalski J,Gabryel B,Herman ZS. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures.Eur Neuropsychopharmacol.2005 Jan;15(1):23-30.
[3]. Lee T,Tang SW. Loxapine and clozapine decreaseserotonin(S2) but do not elevatedopamine(D2)receptornumbers in the rat brain.Psychiatry Res.1984 Aug;12(4):277-85.
| Cell experiment [1]: | |
|
Cell lines |
Rat glial and microglial cells |
|
Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
0.2, 2 and 20 μM; 1 and 3 days |
|
Applications |
In LPS-activated rat mixed glial and microglial cell cultures, Loxapine at all indicated concentrations reduced IL-1β secretion. Besides, Loxapine also reduced IL-2 secretion in mixed glia cultures. In addition, in LPS-induced microglia cultures, Loxapine decreased both IL-1β and IL-2 secretion at the concentrations of 0.2, 2 and 20 μM after the exposure of 1 and 3 days. |
| Animal experiment [2]: | |
|
Animal models |
Wistar rats |
|
Dosage form |
5 mg/kg; i.p. |
|
Applications |
In Wistar rats, chronic administration of Loxapine for 4 weeks or 10 weeks did not increase striatal dopamine receptor density. However, Loxapine significantly reduced cortical serotonin receptor density by 50 ~ 60%. In addition, a single dose of Loxapine exhibited the same potent effect. The results suggested that Loxapine exerted its effect via the serotonin system. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Labuzek K1,Kowalski J,Gabryel B,Herman ZS. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures.Eur Neuropsychopharmacol.2005 Jan;15(1):23-30. [2]. Lee T,Tang SW. Loxapine and clozapine decreaseserotonin(S2) but do not elevatedopamine(D2)receptornumbers in the rat brain.Psychiatry Res.1984 Aug;12(4):277-85. | |
| Cas No. | 1977/10/2 | SDF | |
| Chemical Name | 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine | ||
| Canonical SMILES | CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl | ||
| Formula | C18H18ClN3O | M.Wt | 327.81 |
| Löslichkeit | DMSO : 66mg/mL | 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. |
||
| 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 | 3.0505 mL | 15.2527 mL | 30.5055 mL |
| 5 mM | 0.6101 mL | 3.0505 mL | 6.1011 mL |
| 10 mM | 0.3051 mL | 1.5253 mL | 3.0505 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *