SCH 58261

Names

[ Name ]:
SCH 58261

[Synonym ]:
7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine
2-(Furan-2-yl)-7-phenethyl-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
SCH58261
SCH 58261

Biological Activity

[Description]:

SCH 58261 is the adenosine A2A receptor competitive antagonist. Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively.target: adenosine A2A receptorIC50: 15 nM [3]in vitro: NK cells were cultured in NK cell media and preincubated with or without 1 uM SCH58261 30 min before simulation with indicated concentrations of IL-18 (R & D Systems) and IL-12p70 (Australian Biosearch) in the presence or absence of NECA (1 uM) or CGS-21680 (100 nM).[1]in vivo: it was demonstrated that the selective antagonist of the A2Areceptor, SCH58261, administered i.p. starting from the early minutes after ischemia induction, reduces ischemic brain damage and neurological deficit 24 h thereafter. vehicle-rats received saline with Tween 80 (1 %) administered (i.p.) .SCH58261 (0.01 mg/kg, i.p.), administered twice/day for 7 days [2]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

Research Areas >> Cancer

[References]

[1]. Paul A. Beavis et al. Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors. Proc Natl Acad Sci U S A, 2013 Sep 3, 110(36): 14711-14716.

[2]. Alessia Melani et al. Time-course of protection by the selective A2Areceptor antagonist SCH58261 after transient focal cerebral ischemia. Neurological Sciences, August 2015, Volume 36, Issue 8, pp 1441-1448.

[3]. Varani K et al. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol, 1996 Apr;117(8):1693-701.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.54g/cm3

[ Molecular Formula ]:
C₁₈H₁₅N₇O

[ Molecular Weight ]:
345.35800

[ Exact Mass ]:
345.13400

[ PSA ]:
100.06000

[ LogP ]:
3.14010

[ Index of Refraction ]:
1.807

[ Storage condition ]:
2-8°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

On the role of adenosine (A)₂A receptors in cocaine-induced reward: a pharmacological and neurochemical analysis in rats.

Psychopharmacol. Ser. 232(2) , 421-35, (2015)

Several studies have suggested the inhibitory control of adenosine (A)2A receptor stimulation in cocaine-induced behavioral actions.A combination of systemic or local drug injections and in vivo neuro...

Endothelial dysfunction impairs vascular neurotransmission in tail arteries.

Neurochem. Int. 80 , 7-13, (2015)

The present study intends to clarify if endothelium dysfunction impairs vascular sympathetic neurotransmission. Electrically-evoked tritium overflow (100 pulses/5 Hz) was evaluated in arteries (intact...

Adenosine A2AR blockade prevents neuroinflammation-induced death of retinal ganglion cells caused by elevated pressure.

J. Neuroinflammation 12 , 115, (2015)

Elevated intraocular pressure (IOP) is a major risk factor for glaucoma, a degenerative disease characterized by the loss of retinal ganglion cells (RGCs). There is clinical and experimental evidence ...