"目錄號: HY-14390

GPCR/G Protein-

LAS101057 是一種有效的，選擇性的，可口服的A2B receptor拮抗劑。

Adenosine Receptor

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Preladenant-Vipadenant-CGS 21680 Hydrochloride-ZM241385-Istradefylline-Tozadenant-SCH 58261-Theophylline-Regadenoson-Capadenoson-IB-MECA-Ticlopidine hydrochloride-2-Cl-IB-MECA-N6-[2-(4-Aminophenyl)ethyl]adenosine-N6-Cyclohexyladenosine-

生物活性

Description

LAS101057 is a potent, selective, and orally efficaciousA2B receptorantagonist.

In Vivo

At 3 mg/kg, LAS101057 is active in preventing methacholine-induced AHR, and at 10 mg/kg it inhibits AHR to methacholine to a level virtually equal to that seen with dexamethasone at 1 mg/kg[1].

References

[1].Paul Eastwood, et al. Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. ACS Med Chem Lett. 2011 Mar 10; 2(3): 213-218.