产品
编 号：F167521
分子式：C17H17FN4O2S
分子量：360.41
分子式：C17H17FN4O2S
分子量：360.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1451994-10-7
产品详情
生物活性：
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
体内研究：
VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model.VU0467485 (3 mg/kg; p.o.) treatment displays that the Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM?h and 4.2 hours, respectively.Animal Model:Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model)
Dosage:1, 3, 10 mg/kg
Administration:Oral administration
Result:Dose-dependently reverses AHL.
Animal Model:Male sprague Dawley rats
Dosage:Oral administration (Pharmacokinetic Analysis)
Administration:3 mg/kg
Result:The Cmax, AUCo-infand elimination t1/2 were 1.2 μM, 3.8 μM?h and 4.2 hours, respectively.
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
体内研究：
VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model.VU0467485 (3 mg/kg; p.o.) treatment displays that the Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM?h and 4.2 hours, respectively.Animal Model:Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model)
Dosage:1, 3, 10 mg/kg
Administration:Oral administration
Result:Dose-dependently reverses AHL.
Animal Model:Male sprague Dawley rats
Dosage:Oral administration (Pharmacokinetic Analysis)
Administration:3 mg/kg
Result:The Cmax, AUCo-infand elimination t1/2 were 1.2 μM, 3.8 μM?h and 4.2 hours, respectively.
产品资料
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