PSB 10 hydrochloride

Modify Date: 2024-01-02 12:51:48

PSB 10 hydrochloride Structure
PSB 10 hydrochloride structure
Common Name PSB 10 hydrochloride
CAS Number 591771-91-4 Molecular Weight 435.13500
Density N/A Boiling Point N/A
Molecular Formula C16H15Cl4N5O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PSB 10 hydrochloride


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].

 Names

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
Synonym More Synonyms

 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
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

 Synonyms

psb 10 hydrochloride