TABLE 2.
Ability to activate phospholipase C and stimulate [3H]IP production of various Bn-receptor ligands in cells containing human Bn receptors
Cells were incubated with 3 μCi/ml myo-[2-3H]inositol for 24 hours, then washed and incubated with unlabeled ligand for 60 minutes at 37°C. [3H] production was determined as described under Materials and Methods. The EC50 for each ligand was the concentration causing half-maximal increase in [3H] production. Data were calculated from the experiments shown in Figs. 3 and 4 using Prism. Results are mean ± S.E.M. from at least four experiments, and >10,000 = EC50 >10,000 nM.
| Ligand | EC50 (nM) |
|||||
|---|---|---|---|---|---|---|
| hBRS-3 |
hGRP-R |
hNMB-R |
||||
| Balb 3T3 | NCI-N417 | Balb 3T3 | HuTu-80 | Balb 3T3 | NCI-H1299 | |
| GRP | >10,000 | >10,000 | 0.70 ± 0.09 | 4.00 ± 0.50 | 716 ± 13 | 27.1 ± 2.6 |
| NMB | >10,000 | >10,000 | 22.8 ± 2.2 | 220 ± 26 | 12.1 ± 1.7 | 1.01 ± 0.01 |
| Peptide #1 | 14.2 ± 0.9 | 6.51 ± 1.17 | 0.02 ± 0.01 | 0.50 ± 0.03 | 1.00 ± 0.04 | 0.70 ± 0.07 |
| MK-5046 | 0.08 ± 0.02 | 0.05 ± 0.01 | >10,000 | >10,000 | >10,000 | >10,000 |
| Bantag-1 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |