PSB 10 hydrochloride (10 mg)

90488733

Potent, highly selective hA₃ receptor antagonist/inverse agonist

435.14

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

Potent and highly selective antagonist for the human adenosine A₃ receptor, with low affinity for the rat A₃ receptor (K_i values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A₁, A_2A and A_2B receptors (K_i values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A₁ and A_2A receptors. Acts as an inverse agonist in the [³⁵S]GTPγS binding assay in hA₃-CHO cells (IC₅₀ = 4 nM). Produces thermal hyperalgesia in mice in vivo.

≥98% (HPLC)

Soluble to 25 mM in DMSO and to 10 mM in ethanol

CC[C@H](C3)N=C1N3C(N(C)C2=C1NC(C4=C(Cl)C(Cl)=CC(Cl)=C4)=N2)=O.Cl

C₁₆H₁₄Cl₃N₅O.HCl

591771-91-4