Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).
説明 | VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM). |
In vitro | VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM [1]. |
In vivo | Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1]. |
別名 | VU152100 |
分子量 | 341.43 |
分子式 | C18H19N3O2S |
CAS No. | 409351-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (131.80 mM)
You can also refer to dose conversion for different animals. 詳細
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