| Identification | Back Directory | [Name]
4-[2-[(6-Amino-9-b-D-ribofuranosyl-9H-purin-2-yl)thio]ethyl]benzenesulfonic acid ammonium salt | [CAS]
2122196-16-9 | [Synonyms]
PSB 0777 ammonium
4-[2-[(6-Amino-9-b-D-ribofuranosyl-9H-purin-2-yl)thio]ethyl]benzenesulfonic acid ammonium salt | [Molecular Formula]
C18H24N6O7S2 | [MDL Number]
MFCD34470348 | [MOL File]
2122196-16-9.mol | [Molecular Weight]
500.549 |
| Hazard Information | Back Directory | [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.
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| [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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