Table 3. Ki values and relative affinities of GHRH antagonists to membrane receptors on rat anterior pituitary cells.
Antagonist
|
|||
---|---|---|---|
No | Code no. | Ki*, nM | Relative affinity† |
Standard antagonist | 4.88 | 1 | |
1 | JV-1-62 | 0.057 | 86 |
2 | JV-1-63 | 0.062 | 79 |
5 | JV-1-88 | 0.070 | 70 |
6 | JV-1-91 | 0.091 | 54 |
7 | JV-1-93 | 0.072 | 68 |
8 | JV-1-87 | 0.33 | 15 |
9 | JV-1-86 | 0.14 | 35 |
13 | JV-1-65 | 0.089 | 55 |
14 | JV-1-67 | 0.090 | 54 |
16 | MZ-J-7-72 | 0.074 | 66 |
17 | MZ-J-7-88 | 0.069 | 71 |
18 | MZ-J-7-89 | 0.081 | 60 |
19 | MZ-J-7-90 | 0.071 | 69 |
20 | MZ-J-7-74 | 0.070 | 70 |
21 | MZ-J-7-78 | 0.073 | 67 |
22 | JV-1-36‡ | 0.079 | 62 |
23 | JV-1-38‡ | 0.085 | 57 |
Dissociation constant of the inhibitor-receptor complex. Values were calculated from duplicate or triplicate determinations
Expressed relative to [Ac-Tyr1, d-Arg2] hGHRH(1-29)NH2 (standard antagonist) = 1.0
Reference compounds