Drug intelligence / Profile preview

SCH58261

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Intraperitoneal, Intravenous, Oral
01

Overview

**SCH58261** is a synthetic, small molecule that acts as a potent and highly selective antagonist of the adenosine A2A receptor, showing more than 50-fold selectivity over other adenosine receptor subtypes. Its principal mechanism involves selective blockade of the adenosine A2A receptor, a G protein-coupled receptor widely expressed in the striatum and other brain regions and peripherally in immune tissues. SCH58261 is widely used as a reference compound in preclinical research and has demonstrated antidepressant, nootropic, neuroprotective, and anti-parkinsonian activity in animal models. It is also being explored for its potential to enhance cancer immunotherapy, particularly as a combination partner with immune checkpoint inhibitors. Poor oral bioavailability limits its clinical development, mainly due to poor absorption and high first-pass hepatic metabolism. SCH58261 is classified as a non-xanthine heterocyclic compound and is structurally a triazolopyrimidine derivative[1][2][4][6][7][8][9].

Other names
2-(2-furanyl)-7-(2-phenylethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine5-amino-7-(2-phenylethyl)-2-(2-furyl)-pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine160098-96-44309023MAH4-(furan-2-yl)-10-(2-phenylethyl)-3,5,6,8,10,11-hexaazatricyclo[7.3.0.0^2,6^]dodeca-1(9),2,4,7,11-pentaen-7-amineLSM-3822LSM3822LSM 3822
02

Targets

ADORA2A (Adenosine A₂A Receptor)

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