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.
Am J Transl Res. 2021 May 15;13(5):4040-4054.
Guanosine ameliorates positive symptoms of schizophrenia via modulating 5-HT 1A and 5-HT 2A receptors
Clozapine purchased from AbMole
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Source | Mol Metab (2017). Figure 2. Clozapine |
| Method | Immunohistochemistry | |
| Cell Lines | whole brain | |
| Concentrations | 0.3 mg/kg | |
| 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 Experiment | |
|---|---|
| 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. |
| Concentrations | 50 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | specific pathogen–free Sprague-Dawley rats |
| Formulation | water |
| Dosages | 10, 30, and 100 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 326.82 |
| Formula | C18H19ClN4 |
| CAS Number | 5786-21-0 |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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