| 产品描述: | VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia |
| 靶点: |
mAChR |
| 体外研究: |
Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs). |
| 体内研究: |
VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD). VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration. Animal Model: Male C57BL6/J mice (8-9 weeks old) 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. |
| 参考文献: |
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. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.102 ml |
15.512 ml |
31.023 ml |
| 5 mM |
0.62 ml |
3.102 ml |
6.205 ml |
| 10 mM |
0.31 ml |
1.551 ml |
3.102 ml |
| 50 mM |
0.062 ml |
0.31 ml |
0.62 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |