PeptideDB

PSB-10 hydrochloride

CAS: 591771-91-4 F: C16H15Cl4N5O W: 435.14

PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. P
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Bioactivity PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice[1][2].
Target Ki: 0.44 nM (hA3AR)
Invitro PSB-10 hydrochloride exhibits a subnanomolar Ki value (Ki=0.43 nM versus [3H]NECA) for A3AR. In addition, R-8 is highly selective (>800-fold) versus the other AR subtypes[1].
In Vivo PSB-10 hydrochloride (50-100 mg/kg; i.p.) dose-dependently decreases hot-plate response latencies in mice[2].
Name PSB-10 hydrochloride
CAS 591771-91-4
Formula C16H15Cl4N5O
Molar Mass 435.14
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Ozola V, et, al. 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorg Med Chem. 2003 Feb 6;11(3):347-56. [2]. Abo-Salem OM, et, al. Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66.