Displacement parameters of test compounds for [3H]TASP0434299 and [3H]AVP binding to membranes expressing the human V1B receptor or membranes prepared from the rat anterior pituitary
Values are expressed as the mean ± S.E.M. of Ki values from three to five experiments performed in duplicate (human V1B) or triplicate (rat anterior pituitary).
| [3H]AVP | [3H]TASP0434299 | |||
|---|---|---|---|---|
| Human V1B | Rat Anterior Pituitary | Human V1B | Rat Anterior Pituitary | |
| Ki | Ki | Ki | Ki | |
| nM | nM | nM | nM | |
| Peptides | ||||
| AVP | 0.280 ± 0.045 | 0.132 ± 0.022 | 0.585 ± 0.047 | 0.362 ± 0.068 |
| LVP | 1.10 ± 0.420 | 0.392 ± 0.092 | 0.948 ± 0.041 | 0.705 ± 0.190 |
| (Deamino-Cys1,Leu4,Lys8)-Vasopressin | 0.446 ± 0.055 | 0.127 ± 0.019 | 0.869 ± 0.115 | 1.40 ± 0.054 |
| [Phenylac1,D-Tyr(Me)2,Arg6.8,Tyr-NH29]-Vasopressin | 2.78 ± 0.159 | 0.241 ± 0.086 | 3.25 ± 0.319 | 2.19 ± 0.391 |
| Nonpeptides | ||||
| TASP0390325 | 0.347 ± 0.061 | 0.185 ± 0.020 | 0.315 ± 0.034 | 0.217 ± 0.058 |
| TASP0233278 | 0.254 ± 0.021 | 0.127 ± 0.010 | 0.592 ± 0.049 | 0.396 ± 0.067 |
LVP, lysine vasopressin.