8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride

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8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride manufacturers
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride Basic information
Product Name:8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride
Synonyms:PSB 10 HYDROCHLORIDE;PSB 10;8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride
CAS:591771-91-4
MF:C16H14Cl3N5O.ClH
MW:435.141
EINECS:
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Mol File:591771-91-4.mol
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride Structure
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride Chemical Properties
storage temp. Desiccate at +4°C
solubility Soluble to 25 mM in DMSO and to 10 mM in ethanol
form Powder
Safety Information
MSDS Information
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride Usage And Synthesis
UsesPSB-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].
Biological ActivityPotent and highly selective antagonist for the human adenosine A 3 receptor, with low affinity for the rat A 3 receptor (K i values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A 1 , A 2A and A 2B receptors (K i values are 4.1, 3.3 and 30 μ M respectively) and > 1800-fold selectivity over rat A 1 and A 2A receptors. Acts as an inverse agonist in the [ 35 S]GTP γ S binding assay in hA 3 -CHO cells (IC 50 = 4 nM). Produces thermal hyperalgesia in mice in vivo .
in vivo

PSB-10 hydrochloride (50-100 mg/kg; i.p.) dose-dependently decreases hot-plate response latencies in mice[2].

storageDesiccate at +4°C
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. DOI:10.1016/s0968-0896(02)00456-x
[2] Abo-Salem OM, et, al. Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66. DOI:10.1124/jpet.103.056036
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride Preparation Products And Raw materials
Tag:8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride(591771-91-4) Related Product Information
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride NECA azd4635 N6,N6-Dimethyladenosine 8-[4-[4-(4-Chlorophenzyl)piperazide-1-sulfonyl)phenyl]]-1-propylxanthine CGS 15943