Ki: 2040?nM (α2A adrenoceptor), 285?nM (α2B adrenoceptor), 55?nM (α2C adrenoceptor)

OPC-28326 enhances endothelial tube formation and promotes microvessel growth. OPC-28326 induces phosphorylation of eNOS and Akt in HAECs in a dose dependent-manner, while it does not affect total amounts of eNOS and Akt. OPC-28326 (1-100?μM) and yohimbine (10-1000?nM) causes a rightward shift in the concentration-response curve of clonidine.

OPC-28326 augments blood flow recovery in murine hindlimb ischemia. OPC-28326 significantly increases the number of histologically detectable capillaries in the ischemic leg. OPC-28326 has no beneficial effects on blood flow recovery in eNOS?/? mice. OPC-28326 (3-30?mg/kg, i.v.) and yohimbine causes dose-dependent rightward shift in the pressor dose-response curve induced by B-HT 920. OPC-28326 does not affect on the mydriasis in rats.