591771-91-4

591771-91-4 structure

Name: PSB 10 hydrochloride
Chemical Name: PSB 10 hydrochloride,8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-onemonohydrochloride
CAS Number: 591771-91-4
Molecular Formula: C₁₆H₁₅Cl₄N₅O
Molecular Weight: 435.13500
Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
Create Date: 2017-12-31 07:13:21
Modify Date: 2024-01-02 12:51:48
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].

Name	PSB 10 hydrochloride,8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-onemonohydrochloride
Synonyms	psb 10 hydrochloride

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.