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. 2004 Jan 30;101(6):1708–1713. doi: 10.1073/pnas.0307288101

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

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