产品
编 号：F405349
分子式：C18H17N3O3S
分子量：355.41
分子式：C18H17N3O3S
分子量：355.41
产品类型
规格
价格
是否有货
1mg
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 612514-42-8
产品详情
生物活性：
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 μM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
体内研究：
VU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats.Animal Model:Male Sprague-Dawley rats (270-300 g) injected with Amphetamine
Dosage:56.6 mg/kg
Administration:i.p.; once
Result:Reversed Amphetamine-induced hyperlocomotion in rats.
体外研究：
VU0152099 (30 μM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 μM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC50 values of 1.2 μM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh.
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 μM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
体内研究：
VU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats.Animal Model:Male Sprague-Dawley rats (270-300 g) injected with Amphetamine
Dosage:56.6 mg/kg
Administration:i.p.; once
Result:Reversed Amphetamine-induced hyperlocomotion in rats.
体外研究：
VU0152099 (30 μM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 μM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC50 values of 1.2 μM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh.
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