VU 0357017 hydrochloride
Cat. No. 4295
Chemical Name: 4-[[2-[(2-Methylbenzoyl)amino]ethyl
Biological ActivityPositive 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.
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Certificate of Analysis / Product Datasheet / Safety Data Sheet
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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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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