VU 0357017 hydrochloride
Positive allosteric modulator of muscarinic M1 receptors (EC50 = 198 nM). Displays no activity at M2-M5 at concentrations up to 30 μM. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant.
|Storage||Store at +4°C|
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 369.89. 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||2.7 mL||13.52 mL||27.04 mL|
|5 mM||0.54 mL||2.7 mL||5.41 mL|
|10 mM||0.27 mL||1.35 mL||2.7 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the biological activity of the product.
Bridges et al (2010) Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) Lead. Part II. Development of potent and highly selective M1 PAM. Bioorg.Med.Chem.Lett. 20 1972 PMID: 20156687
Lebois et al (2010) Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system. ACS Chem.Neurosci. 1 104
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1 Citation for VU 0357017 hydrochloride
Citations are publications that use Tocris products. Selected citations for VU 0357017 hydrochloride include:
Jadeja et al (2016) Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress. J Am Soc Nephrol 6 405 PMID: 26862589
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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
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
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.