Description: Muscarinic receptor ligand; exhibits partial agonist and antagonist activity at different subtypes
Chemical Name: (1R,5R,6R)-6-[4-(Propylthio)-1,2,5-thiadiazol-3-yl]-1-azabicyclo[3.2.1]octane oxalate
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Raedleret al (2007) Towards a muscarinic hypothesis of schizophrenia. Mol.Psychiatry 12 232 PMID: 17146471
Shannonet al (1999) Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats. J.Pharmacol.Exp.Ther. 290 901 PMID: 10411607
Bymasteret 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