PSB-10

PSB-10
Systematic (IUPAC) name
(8R)-ethyl-4-methyl-2-(2,3,5-trichlorophenyl)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]purin-5-one
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
ATC code  ?
Synonyms PSB-10
Chemical data
Formula C16H16Cl3N5O 
Mol. mass 400.690 g/mol
SMILES eMolecules & PubChem
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PSB-10 is a drug which acts as a selective inverse agonist[1] for the adenosine A3 receptor, with high selectivity over the other three adenosine receptor subtypes. It has been shown to produce antiinflammatory effects in animal studies.[2] Simple xanthine derivatives such as caffeine and DPCPX have generally low affinity for the A3 subtype and must be extended by expanding the ring system and adding an aromatic group to give high A3 affinity and selectivity.[3]

References

  1. ^ Hallmen C, Wiese M (2006). "Molecular dynamics simulation of the human adenosine A3 receptor: agonist induced conformational changes of Trp243". Journal of Computer-aided Molecular Design 20 (10-11): 673–84. doi:10.1007/s10822-006-9088-5. PMID 17124628. 
  2. ^ Bilkei-Gorzo A, Abo-Salem OM, Hayallah AM, Michel K, Müller CE, Zimmer A (March 2008). "Adenosine receptor subtype-selective antagonists in inflammation and hyperalgesia". Naunyn-Schmiedeberg's Archives of Pharmacology 377 (1): 65–76. doi:10.1007/s00210-007-0252-9. PMID 18188542. 
  3. ^ Müller CE (2003). "Medicinal chemistry of adenosine A3 receptor ligands". Current Topics in Medicinal Chemistry 3 (4): 445–62. doi:10.2174/1568026033392174. PMID 12570761. http://www.bentham-direct.org/pages/content.php?CTMC/2003/00000003/00000004/0008R.SGM. 
Receptor ligands
2-(1-Hexynyl)-N-methyladenosine • 2-Cl-IB-MECA • 2'-MeCCPA • 5'-N-ethylcarboxamidoadenosine • ATL-146e • BAY 60–6583 • CCPA • CGS-21680 • CP-532,903 • GR 79236 • LUF-5835 • LUF-5845 • N6-Cyclopentyladenosine • Regadenoson • SDZ WAG 994 • UK-432,097
8-Phenyl-1,3-dipropylxanthine • Acefylline • Aminophylline • Bamifylline • Caffeine • CGS-15943 • 8-Chlorotheophylline • CPX • CVT-6883 • Dimethazan • DPCPX • Fenethylline • Istradefylline • KF-26777 • MRE3008F20 • MRS-1220 • MRS-1334 • MRS-1706 • MRS-1754 • MRS-3777 • Paraxanthine • Pentoxifylline • Preladenant • Propentofylline • PSB-10 • PSB-11 • PSB 36 • PSB-603 • PSB-788 • PSB-1115 • Rolofylline • SCH-442,416 • SCH-58261 • Theobromine • Theophylline • VUF-5574 • ZM-241,385
Reuptake inhibitors
ENT inhibitors
VNT inhibitors