Binding affinity of SSR149415 for vasopressin and oxytocin receptors in animal and human species
| Ki | ||||
|---|---|---|---|---|
| V1b | V1a | V2 | OT | |
| nM | ||||
| Human | ||||
| Hypophysis | 4.2 ± 1.1 | |||
| CHO | 1.5 ± 0.8 | |||
| CHO | 91 ± 23 | |||
| CHO | 1412 ± 314 | |||
| Ltk− | 174 ± 35 | |||
| Rat | ||||
| Hypophysis | 3.7 ± 1.3 | |||
| CHO | 1.3 ± 0.9 | |||
| Liver | 1050 ± 112 | |||
| Kidney | 2897 ± 509 | |||
| Mammary | 270 ± 39 | |||
| Bovine | ||||
| Hypophysis | 2.7 ± 0.8 | |||
Binding assays were performed as described under Experimental Procedures using either CHO/Ltk− cells transfected with the corresponding AVP/OT receptor or native tissues constitutively expressing this receptor. Inhibition constants (Ki) were determined from competition experiments and calculated according to the Cheng and Prusoff (1973) equation. Values are mean ± S.D. of at least three determinations.