AH23848

AH23848 (compound 6) is a competitive blocker of the thromboxane A₂ receptor and an orally effective agent, with an IC₅₀ value of 50 nM against human targets and a long duration of action. AH23848 shows no activity against other prostaglandin, serotonin (5-HT) or adenosine diphosphate (ADP) receptors. AH23848 can be used in the research of occlusive vascular diseases^[1]. In Vitro:AH23848 (compound 6) (3.0×10^-8-3.0×10^-6 mol/liter; 30 min) acts as a competitive antagonist of thromboxane A₂ receptors in isolated human pulmonary artery smooth muscle with a pA₂ of 7.8^[1].
AH23848 (6.0×10^-8-6.0×10^-6 mol/liter; 1.0×10^-5 mol/liter) competitively antagonizes thromboxane A₂ receptors in isolated rat aorta smooth muscle with a pA₂ of 7.94, and does not block 5-HT or potassium chloride-induced contractions at concentrations up to 1.0×10^-5 mol/liter^[1].
AH23848 (1.0×10⁻⁶ mol/liter) does not block PGE₂- or PGF₂α-induced contractions in isolated non-vascular smooth muscle preparations^[1].
AH23848 (1.0×10^-7-1.0×10^-4 mol/liter) potently and specifically inhibits thromboxane receptor-dependent platelet aggregation in human platelet-rich plasma, with IC₅₀ values ranging from 1.05×10^-7 to 6.3×10^-7 mol/liter for different agonists, and does not block ADP-, 5-HT-, or epinephrine-induced aggregation^[1]. In Vivo:AH23848 (0.03-1.0 mg/kg; i.v.; single bolus) potently and specifically inhibits collagen-induced thromboembolic and bronchoconstrictor responses in anesthetized guinea pigs, with no effect on ADP-induced thrombocytopenia at doses up to 1.0 mg/kg i.v^[1].
AH23848 (0.01-0.3 mg/kg; i.v.; single bolus) specifically antagonizes U-46619-induced mesenteric vasoconstriction in anesthetized Beagle dogs without altering baseline hemodynamic parameters, with a 6.5-fold rightward shift of the U-46619 dose-response curve at 0.1 mg/kg i.v^[1].
AH23848 (1 mg/kg; p.o.; single dose) produces sustained, specific inhibition of collagen-induced platelet aggregation in conscious Beagle dogs, with peak effects showing a 23-fold rightward shift of the collagen dose-response curve and residual activity lasting at least 11 hours^[1].