Table 3.
Effects of cytotoxic SST hybrid AN-238 and its carrier analog RC-121 on hGH-RH(1-29)NH2 or forskolin-induced GH-release in dispersed rat pituitary superfusion system in vitro
| Compound | Exposure time, min | GH response, ng
|
Inhibition (%) | GH response, ng
|
Inhibition (%) | ||
|---|---|---|---|---|---|---|---|
| Control | RC-121 | Control | AN-238 | ||||
| 1 nM GH-RH + 1 nM analog | 3 | 560 | 22 | 96 | 493 | 80 | 84 |
| 1 nM GH-RH + 1 nM analog | 30 | 2,598 | 0 | 100 | 1,939 | 101 | 95 |
| 0.2 nM GH-RH + 0.1 nM analog | 6 | 260 | 0 | 100 | 214 | 23 | 91 |
| 0.2 nM GH-RH + 0.5 nM analog | 6 | 277 | 0 | 100 | 215 | 18 | 92 |
| 4 μM forskolin + 0.5 nM analog | 6 | 760 | 90 | 88 | 760 | 230 | 70 |
| 10 μM forskolin + 2 nM analog | 6 | 696 | 294 | 58 | 554 | 258 | 54 |
Cells were exposed to the secretagogues alone or in combination with the SST analogs for different duration and at various concentrations. The GH-release inhibitory activities of the analogs are expressed as relative GH-releasing potencies (ng, “net integral” values) of the secretagogues administered with or without the analogs.