VU0453595 Chemical Properties

Boiling point:

552.8±50.0 °C(Predicted)

Density 

1.35±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 100 mg/mL (310.23 mM; Need ultrasonic)

form 

Solid

pka

2.98±0.20(Predicted)

color 

Off-white to light yellow

VU0453595 Usage And Synthesis

Biological Activity

VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia[1][2]. Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs)[3]. VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD)[1].VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration[1].

References

[1]. A Ghoshal, et al. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology. 2016 Jan;41(2):598-610. [2]. Sean P Moran, et al. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. [3]. Xiaohui Lv, et al. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222.

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