Biological Activity
Atypical antipsychotic drug, with a much lower tendency to cause extrapyramidal side effects than conventional neuroleptics. Displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade (Ki values are 21, 170, 170, 230 and 330 nM for D4, D3, D1, D2 and D5 receptors respectively).
Technical Data
| M. Wt | 326.83 |
| Formula | C18H19ClN4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 5786-21-0 |
| PubChem ID | 2818 |
| InChI Key | ZUXABONWMNSFBN-UHFFFAOYSA-N |
| Smiles | CN1CCN(CC1)C1=NC2=C(NC3=C1C=CC=C3)C=CC(Cl)=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 2eq.HCl | 16.34 | 50mM with gentle warming | |
| DMSO | 32.68 | 100 | |
| ethanol | 16.34 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 326.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.06 mL | 15.3 mL | 30.6 mL |
| 5 mM | 0.61 mL | 3.06 mL | 6.12 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.06 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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References
References are publications that support the products' biological activity.
Canton et al (1990) Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites. Eur.J.Pharmacol. 191 93 PMID: 1982659
Ellenbroek et al (1991) The involvement of dopamine D1 and D2 receptors in the effects of the classical neuroleptic haloperidol and the atypical neuroleptic clozapine. Eur.J.Pharmacol. 196 103 PMID: 1678712
Seeman and Van Tol (1994) Dopamine receptor pharmacology. Trends Pharmacol.Sci. 15 264 PMID: 7940991
Jensen et al (2013) Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-dazepin-3-ol analogues: novel 5-HT2A/5-HT2C receptor agonists with pro-cognitive J.Med.Chem. 56 1211 PMID: 23301527
Keywords: Clozapine, supplier, Dopamine, antagonists, D4, selectivity, 5HT2A/2C, Non-Selective, Receptors, Serotonin, 5HT2C, 5HT2, 5HT2A, dopaminergic, Non-selective, Dopamine, 5-HT2A, Receptors, 5-HT2C, Receptors, Non-selective, Dopamine, Tocris Bioscience
