VU 0357017 hydrochloride
Chemical Name: 4-[[2-[(2-Methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid ethyl ester hydrochloride
Purity: ≥98%
Biological Activity
VU 0357017 hydrochloride is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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.
Bridges et al.
Bioorg.Med.Chem.Lett., 2010;20:1972 -
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system.
Lebois et al.
ACS Chem.Neurosci., 2010;1:104
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Citations for VU 0357017 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for VU 0357017 hydrochloride include:
3 Citations: Showing 1 - 3
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Muscarinic M1 Receptors Modulate Working Memory Performance and Activity via KCNQ Potassium Channels in the Primate Prefrontal Cortex.
Authors: Pasko Et al.
Neuron 2020;106:649-661.e4
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Muscarinic M1 Receptor Overstimulation Disrupts Working Memory Activity for Rules in Primate Prefrontal Cortex.
Authors: Stefan Et al.
Neuron 2018;98:1256-1268.e4
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Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress.
Authors: Jadeja Et al.
J Am Soc Nephrol 2016;6:405
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