| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140?nM) for the research of schizophrenia[1][2]. | [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]. | [in vivo]
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]. | Animal Model: | Male C57BL6/J mice (8-9 weeks old)[1] | | Dosage: | 1, 3, or 10?mg/kg | | Administration: | Intraperitoneal (i.p.); 10?mL/kg; administered 30?min before the social interaction test | | Result: | Rescued deficits in social interaction observed in PCP-treated mice. |
| [storage]
Store at -20°C | [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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