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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
References are publications that support the biological activity of the product.
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
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Keywords: PTAC oxalate, PTAC oxalate supplier, PTAC, antipsychotics, schizophrenia, selective, muscarinic, partial, agonists, antagonists, M1, M2, M3, M4, M5, Non-selective, Muscarinics, 4533, Tocris Bioscience
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Learning & Memory Poster
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.