Table 1. Peptides inhibition constants (Ki in nM).
Human OTR | Human V1a | Human V1b | Human V2 | |
---|---|---|---|---|
LVT | 2.40±0.425 | 30.8±4.2 | 24.9±7.3 | 2593±625 |
dLVT | 3.88±0.585 | 35.5±6.2 | 71.7±2.0 | 3737±400 |
DOTA-dLVT | 1.21±0.199 | 370±58 | 640±177 | 3562±280 |
Binding of LVT-derived peptides to human OT/AVP receptor subtypes. Competition experiments were performed using membrane preparations of COS7 cells transiently transfected with the wild-type human OTR, and V1a, V1b and V2 receptors. The Ki values for the human OTR were obtained by displacement of [3H]-OT; the Ki values for the human V1a, V1b and V2 receptors were obtained by displacement of [3H]-AVP. The values are the mean values±s.e. of three different experiments each performed in triplicate.