Biological Activity
Muscarinic receptor ligand. Displays partial agonist activity at M2 and M4 receptors; exhibits antagonist effects at M1, M3 and M5 receptors (Ki values are 2.8, 0.2, 0.6, 0.2 and 0.8 nM respectively). Displays selectivity for muscarinic receptors over a range of neurotransmitter receptors and ion channels. Inhibits firing rate of dopaminergic cells in the limbic ventral tegmental area after acute administration, without binding to dopamine receptors.
Technical Data
| M. Wt | 359.46 |
| Formula | C12H19N3S2.C2H2O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 201939-40-4 |
| PubChem ID | 90488949 |
| InChI Key | LXXQOVMTAFXOKQ-IYPAPVHQSA-N |
| Smiles | CCCSC1=NSN=[C@]1[C@@H]2[C@H]3CCCN(C3)C2.O=C(C(O)=O)O |
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 | |||
| DMSO | 35.95 | 100 | |
| ethanol | 35.95 | 100 | |
| water | 35.95 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 359.46. 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 | 2.78 mL | 13.91 mL | 27.82 mL |
| 5 mM | 0.56 mL | 2.78 mL | 5.56 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Raedler et al (2007) Towards a muscarinic hypothesis of schizophrenia. Mol.Psychiatry 12 232 PMID: 17146471
Shannon et al (1999) Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats. J.Pharmacol.Exp.Ther. 290 901 PMID: 10411607
Bymaster et al (1998) Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane. Eur.J.Pharmacol. 356 109 PMID: 9774240
Keywords: PTAC oxalate, supplier, PTAC, antipsychotics, schizophrenia, selective, muscarinic, partial, agonists, antagonists, M1, M2, M3, M4, M5, Non-selective, Muscarinics, Non-selective, Muscarinics, Tocris Bioscience
