Table 1.
The potency of ML290 and relaxin in HEK-RXFP1 and human primary vascular cells for p-ERK1/2, pp38MAPK, cGMP and cAMP accumulation.
| p-ERK1/2 (% 10% FBS) | p-p38MAPK (% sorbitol) | |||
|---|---|---|---|---|
| H2 relaxin | ML290 | H2 relaxin | ML290 | |
| HEK-RXFP1 | 9.5 ± 0.3 (4) (31.8 ± 1.7) | NE (8) | 8.9 ± 0.3 (4) (29.8 ± 1.7) | 9.3 ± 0.6 (6) (16.9 ± 2.2) |
| HCAEC | ND | NE (3) | ND | NE (3) |
| HUVEC | 9.2 ± 0.3# (5) (11.2 ± 2.7) | NE (3) | ND | NE (3) |
| HUASMC | 9.1 ± 0.4# (6) (27.7 ± 8.1) | NE (3) | ND | 8.6 ± 0.6 (3) (4.4 ± 1.6) |
| HUVSMC | 9.2 ± 0.4# (6) (15.2 ± 4.4) | NE (3) | ND | 8.5 ± 1.0 (3) (2.7 ± 0.9) |
| HCF | 9.1 ± 0.3# (5) (54.7 ± 15.9) | NE (3) | ND | ND |
| cGMP (% DEA 1 μM) | cAMP (% forskolin 50 μM) | |||
| HEK-RXFP1 | NE (3) | NE (3) | 10.3 ± 0.1 (5) (129.0 ± 5.8) | 6.4 ± 0.1 (6) (113.3 ± 1.8) |
| HCAEC | 9.2 ± 0.5 (3) (39.6 ± 14.8) | 7.2 ± 0.4 (7) (40.6 ± 5.6) | 8.9 ± 0.5 (3) (13.0 ± 5.2) | 6.1 ± 0.3 (7) (17.9 ± 3.3) |
| HUVEC | 8.9 ± 0.4# (7) (65.4 ± 19.8) | 7.3 ± 0.5 (7) (23.5 ± 4.4) | 9.1 ± 0.4# (9) (6.0 ± 2.7) | 6.2 ± 0.7 (7) (11.7 ± 3.9) |
| HUASMC | 9.1 ± 0.3# (6) (55.7 ± 12.4) | 7.2 ± 0.5 (7) (21.0 ± 4.1) | 9.0 ± 0.3# (7) (4.5 ± 1.6) | 6.2 ± 0.5 (5) (11.9 ± 3.9) |
| HUVSMC | 9.2 ± 0.4# (6) (31.4 ± 10.9) | 7.2 ± 0.6 (4) (11.0 ± 3.4) | 9.6 ±0.4# (10) (5.1 ± 1.8) | 6.1 ± 0.5 (4) (10.8 ± 3.0) |
| HCF | 9.6 ± 0.7 (5) (62.3 ± 7.6) | 7.5± 0.3 (5) (45.3 ± 4.1) | NE (3) | ND |
Note: #Indicates data taken from our previous publication conducted in the same cells6. Efficacy (below in brackets) expressed as a % of control responses for each pathway. N numbers in brackets. NE – no effect; ND – not determined.