PSB36

PSB36 is a highly selective A₁ adenosine receptor antagonist, with a K_i of 0.12 nM and a K_d of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD₉₀ of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation^[1][2][3]. In Vitro:PSB36 (1 μM; 10 min) significantly prolongs APD₉₀ in intact trabeculae isolated from human right atrial appendages from patients in sinus rhythm^[3]. In Vivo:PSB36 (30-100 mg/kg; i.p.) produces no analgesic effect in the mouse hot plate model of acute thermal pain^[1].
Systemic administration of PSB36 (10-100 mg/kg; i.p.; single dose) significantly reduces formalin-induced hind paw edema and early phase inflammatory pain, whereas no such effect is observed with local administration^[2].
Systemic administration of PSB36 (10-100 mg/kg; i.p.; single dose) significantly reduces carrageenan-induced hind paw edema^[2].