PSB 10 hydrochloride

Names

[ Name ]:
PSB 10 hydrochloride

[Synonym ]:
psb 10 hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

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

[Target]

Ki: 0.44 nM (hA3AR)[2]

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₅Cl₄N₅O

[ Molecular Weight ]:
435.13500

[ Exact Mass ]:
433.00300

[ PSA ]:
67.97000

[ LogP ]:
3.62080

Related Compounds

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