Clozapine (Clozaril) is a potent 5-HT1C receptor antagonist with an IC50 of 110 nM for 5-HT-stimulated phosphoinositide hydrolysis. It is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Clozapine is classified as an atypical antipsychotic compound because its profile of binding to serotonergic as well as dopamine receptors; its effects on various dopamine mediated behaviors also differ from those exhibited by more typical antipsychotics.
|Source||Mol Metab (2017). Figure 2. Clozapine|
|Cell Lines||whole brain|
|Incubation Time||0.5 h|
|Results||We found in Figure 2 that hM3Dq-mCherry (in red) was expressed in the brainstem NTS-DMV, and upon ip injection of clozapine-N-oxide (CNO, 0.3 mg/kg), hM3Dq-mediated activation of Gcgþ neurons induced an abundant expression of the early response gene c-Fos (in green, C) in the brainstem NTS-DMV and AP compared to that in A, suggesting activation of Gcgþ neurons-mediated neural circuitry.|
|Cell lines||A549 and H1299 human NSCLC cells|
|Preparation method||Residual CFSE was then removed by washing twice with phosphate-buffered saline (PBS), followed by cell growth in culture medium with or without 50 μM clozapine for 72 h. For cell cycle analysis, cells were fixed in 70% ethanol and stained with a PI/Triton X-100 DNA-staining solution (20 μg/mL PI, 0.1% Triton X-100, and 0.2 mg/mL RNase A in PBS) at room temperature for 30 min.|
|Incubation time||72 h|
|Animal models||specific pathogen–free Sprague-Dawley rats|
|Dosages||10, 30, and 100 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
The Drug-Drug Effects of Rhein on the Pharmacokinetics and Pharmacodynamics of Clozapine in Rat Brain Extracellular Fluid by In Vivo Microdialysis.
Hou ML, et al. J Pharmacol Exp Ther. 2015 Oct;355(1):125-34. PMID: 26220937.
Clozapine induces autophagic cell death in non-small cell lung cancer cells.
Yin YC, et al. Cell Physiol Biochem. 2015;35(3):945-56. PMID: 25659606.
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