Agonists | Endogenous ligands (human): |
| GHRH(1–44)NH2, GHRH(1–40)OH, GHRH(1–37)NH2
|
| Selective agonists (only a few representative compounds are listed): |
| Standard GHRH(1–29)NH2
|
| BIM 28011 | [D-Ala2, Ala8,9,15,27, D-Arg29]hGHRH(1–29)NH2 (Coy et al., 1996) |
| NC-9-96 | [D-Ala2, Aib8,18,24, Ala9,15,16,18,22,24–28]hGHRH(1–29)NH2(Coy et al., 1996) |
| Standard hGHRH(1–40)OH |
| No. 15 | [Ala15, Nle27]hGHRH(1–29)NH2 (Cervini et al., 1998) |
| No. 29 | [MeTyr1, Ala15,22, Nle27]hGHRH(1–29)NH2(Cervini et al., 1998) |
| No. 46 | Cyclo(25–29)[MeTyr1, Ala15, D-Asp25, Nle27, Orn29] hGHRH(1–29)NH2 (Cervini et al., 1998) |
Agonist potencies | GHRH(1–29)NH2
| 1.0 |
| BIM 28011 | 4.9 |
| NC-9-96 | 2.6 |
| hGHRH(1–40)OH | 1.0 |
| No. 15 | 5.6 |
| No. 29 | 25.6 |
| No. 26 | 16.7 |
| Relative growth hormone-releasing potency in vitro on rat pituitary cell cultures compared to either the GHRH(1–29)NH2 (Coy et al., 1996) or hGHRH(1–40)OH (Cervini et al., 1998) standards |
Antagonists | Only a few representative compounds are listed: |
| Standard | [Ac-Tyr1, D-Arg2]hGHRH(1–29)NH2 (Robberecht et al., 1985) |
| MZ-4-71 | [Ibu-Tyr1, D-Arg2, Phe(4-Cl)6, Abu15, Nle27]hGHRH(1–28)Agm (Zarandi et al., 1994) |
| MZ-5-156 | [PhAc-Tyr1, D-Arg2, Phe(4-Cl)6, Abu15, Nle27]hGHRH(1–28)Agm (Zarandi et al., 1994) |
| JV-1-36 | [PhAc-Tyr1, D-Arg2, Phe(4-Cl)6, Arg9, Abu15, Nle27, D-Arg28, Har29]hGHRH(1–29)NH2 (Schally and Varga, 1999) |
| JV-1-38 | [PhAc-Tyr1, D-Arg2, Phe(4-Cl)6, Har9, Tyr(Me)10, Abu15, Nle27, D-Arg28, Har29]hGHRH(1–29)NH2(Schally and Varga, 1999) |
Antagonist | [Ac-Tyr1, D-Arg2]hGHRH(1–29)NH2
| 52% 3.22 nM |
potencies | MZ-4-71 | 83% 0.12 nM |
| MZ-5-156 | 95% 0.069 nM |
| JV-1-36 | 100% 0.042 nM |
| JV-1-38 | 98% 0.079 nM |
| Inhibition of in vitro growth hormone release induced by 1 nM hGHRH(1-29)NH2 by 30 nM antagonist, and dissociation constant of the inhibitor-receptor complex (Schally and Varga, 1999) |