VU6005649 |
| カタログ番号GC19381 |
VU6005649 は、CNS 浸透 mGlu7/8 受容体アゴニストであり、mGlu7 受容体と mGlu8 受容体の EC50 はそれぞれ 0.65 μM と 2.6 μM です。
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Cas No.: 2137047-43-7
Sample solution is provided at 25 µL, 10mM.
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VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 uM and 2.6 uM for mGlu7 receptor and mGlu8 receptor, respectively.
VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 uM and 2.6 uM for mGlu7 receptor and mGlu8 receptor, respectively. VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50[1].
When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H2O (0.75 mg/kg. s.c. amphetamine), no efficacy is observed in this assay. VU6005649 shows modest but significant pro-cognitive effects on associative learning in wild-type mice and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model[1].
References:
[1]. Abe M, et al. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115.
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