ChemicalBook CAS DataBase List 2122196-16-9

2122196-16-9

Name	4-[2-[(6-Amino-9-b-D-ribofuranosyl-9H-purin-2-yl)thio]ethyl]benzenesulfonic acid ammonium salt
CAS	2122196-16-9
Molecular Formula	C18H24N6O7S2
MDL Number	MFCD34470348
Molecular Weight	500.549
MOL File	2122196-16-9.mol

Chemical Properties

solubility

Soluble to 100 mM in water and to 100 mM in DMSO

Hazard Information

Description

PSB-0777 is an Adenosine A 2A Receptor Agonist

Uses

PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research[1][2][3].

in vivo

PSB 0777 ammonium (0.4 mg/kg/day; oral gavage; from the day 5 to 10) causes a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture^[3].
PSB 0777 ammonium (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice^[2].
PSB 0777 ammonium cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium (0.4 mg/kg/day; PO) has very low plasma concentrations in rats at 30 min (below 5 nM), and there is no plasma concentrations at 60 min after administration. PSB 0777 ammonium (0.4 mg/kg/day; IP) makes plasma concentrations well evident at 30 min, and decreases after 60 min, and is not detectable at 120 and 240 min^[3].

Animal Model:	Albino male Sprague-Dawley rats of 200 g with Oxazolone-induced colitis^[3]
Dosage:	0.4 mg/kg
Administration:	Oral gavage; daily; from the day 5 to 10
Result:	Caused a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture alone or in combination with Dexamethasone (1 mg/kg/day). Counteracted significantly the increment of colonic myeloperoxidase (MPO) levels associated with colitis.

storage

Store at RT

References

[1] Ali El-Tayeb, et al. Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists. ACS Med Chem Lett. 2011 Oct 10;2(12):890-5. DOI:10.1021/ml200189u
[2] Jesse Lea Carlin, et al.Activation of adenosine A 2A or A 2B receptors causes hypothermia in mice. Neuropharmacology. 2018 Sep 1;139:268-278. DOI:10.1016/j.neuropharm.2018.02.035
[3] L Antonioli, et al. Anti-inflammatory effect of a novel locally acting A 2A receptor agonist in a rat model of oxazolone-induced colitis. Purinergic Signal. 2018 Mar;14(1):27-36. DOI:10.1007/s11302-017-9591-2

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