VU0453595 是一种高选择性、全身活性的 M1 正变构调节剂 (PAM, EC50=2140 nM)，可用于精神分裂症的研究[1]。
货号:ajcx35328
CAS:1432436-13-9
分子式:C18H15FN4O
分子量：322.34
溶解度:DMSO : 100 mg/mL (310.23 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.