1876450-21-3

KD: 300 nM (apelin receptor in CHO-K1 cells), 172 nM (apelin receptor in human heart).

MM 07 competes with nanomolar affinities for binding of [Glp ⁶⁵ ,Nle ⁷⁵ ,Tyr ⁷⁷ ] [ ¹²⁵ I]apelin-13 to human apelin receptors in CHO-K1 cells (K _D , 300 nM) and human heart (K _D , 172 nM, n=3).

MM 07 causes a dose-dependent increase in cardiac output, and although there is a decrease in vascular resistance, this is without corresponding effects on BP. Administration of SNAP produces a profound fall in BP in both [Pyr ¹ ]apelin-13 and MM 07-treated groups; however, although cardiac output is significantly increased in response to SNAP in the MM 07 group, it is significantly reduced in the [Pyr ¹ ]apelin-13 group. Neither peptide causes a significant change in heart rate, respiratory rate, or temperature. Both [Pyr ¹ ]apelin 13 and MM 07 increases peak velocity above basal levels.