VU0467485 (Synonyms: AZ13713945) |
| Catalog No.GC38957 |
VU0467485(AZ13713945)는 강력하고 선택적이며 경구 생체이용 가능한 무스카린성 아세틸콜린 수용체 4(M4) 양성 알로스테릭 조절제(PAM)입니다.
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Cas No.: 1451994-10-7
Sample solution is provided at 25 µL, 10mM.
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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[1].
VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model[1].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[1]. Animal Model: Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model) [1]
[1]. Wood MR, et al. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. ACS Med Chem Lett. 2016 Dec 16;8(2):233-238.
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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