Human growth hormone-releasing hormone hGHRH(1-29)-NH2: systematic structure-activity relationship studies.

Cervini LA, Donaldson CJ, Koerber SC, Vale WW, Rivier JE

Journal of medicinal chemistry1 Feb 1998Cited by 17 (Europe PMC)

PMID9513600DOI10.1021/jm970618sPepBankPUB-09513600

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study8

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone8

In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Sermorelin.

01LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
In vitro, alanine-substituted analogs of hGHRH(1-29)-NH2 at positions 8, 9, 15, 22 and 28 were 2-6 times more potent than the hGHRH(1-40)-OH standard.
In plain wordsIn lab tests, several modified versions of GHRH(1-29) were 2 to 6 times more potent than the standard.
Peptide
Sermorelin
Outcome
IncreasePotency of alanine-substituted analogs
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Measurements
Relative potency
2 to 6 times standard
single alanine analogs
Source sentences
Summary
Single-point replacement of each amino acid by alanine led to the identification of [Ala8]-, [Ala9]-, [Ala15]- (Felix et al. Peptides 1986 1986, 481), [Ala22]-, and [Ala28, Nle27]-hGHRH(1-29)-NH2 as being 2-6 times more potent than hGHRH(1-40)-OH (standard) in vitro.
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360001
02LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
In vitro, alanine replacement at many positions of hGHRH(1-29)-NH2 caused nearly complete loss of potency, whereas some gave equipotent analogs and others weak agonists.
In plain wordsIn lab tests, changing many single amino acids of GHRH(1-29) almost wiped out its activity, while a few changes kept it.
Peptide
Sermorelin
Outcome
MixedPotency loss in alanine scan analogs
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Source sentences
Summary
Nearly complete loss of potency was seen for [Ala1], [Ala3], [Ala5], [Ala6], [Ala10], [Ala11], [Ala13], [Ala14], and [Ala23], whereas [Ala16], [Ala18], [Ala24], [Ala25], [Ala26], and [Ala29] yielded equipotent analogues and [Ala7], [Ala12], [Ala17], [Ala20], [Ala21], and [Ala27] gave weak agonists w…
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360002
03LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
In vitro, two multiple-alanine-substituted hGHRH(1-29)-NH2 analogs released growth hormone 26 and 11 times more effectively than the standard.
In plain wordsIn lab tests, two heavily modified GHRH(1-29) versions released growth hormone 26 and 11 times more effectively than the standard.
Peptide
Sermorelin
Outcome
IncreasePotency of multiple-alanine analogs
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Measurements
Relative potency
26 times standard
analog 29
Relative potency
11 times standard
analog 30
Source sentences
Summary
The multiple-alanine-substituted peptides [MeTyr1,Ala15,22,Nle27]-hGHRH(1-29)-NH2 (29) and [MeTyr1,Ala8,9,15,22,28,Nle 27]-hGHRH(1-29)-NH2 (30) released growth hormone 26 and 11 times, respectively, more effectively than the standard in vitro.
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360003
04LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
In vitro, Aib substitution of the nine most potent alanine analogs gave similar results to the alanine analogs, except [Aib8] (doubling versus [Ala8]), [Aib9] (the abstract text reads 'having' versus [Ala9]) and [Aib15] (10-fold decrease versus [Ala15]).
In plain wordsIn lab tests, swapping in a different helix-promoting amino acid mostly gave similar potency to the alanine versions, but a few differed, one 10-fold weaker.
Peptide
Sermorelin
Outcome
MixedPotency of Aib-substituted analogs
Study
n: not reported in source
Comparator
Alanine-substituted analogs
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Source sentences
Summary
Individual substitution of the nine most potent peptides identified from the Ala series with the helix promoter alpha-aminoisobutyric acid (Aib) produced similar results, except for [Aib8] (doubling vs [Ala8]), [Aib9] (having vs [Ala9]), and [Aib15] (10-fold decrease vs [Ala15]).
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360004
05LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
In vitro, the cyclic lactam-constrained analog 46 of hGHRH(1-29)-NH2 was 17 times more potent than the standard.
In plain wordsIn lab tests, a ring-shaped version of GHRH(1-29) was 17 times more potent than the standard.
Peptide
Sermorelin
Outcome
IncreasePotency of cyclic analog 46
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Measurements
Relative potency
17 times standard
analog 46
Source sentences
Summary
Application of lactam constraints in the C-terminus of GHRH(1-29)-NH2 identified cyclo(25-29)[MeTyr1,Ala15,DAsp25,Nle27,Orn29+ ++]-hGHRH(1-29)-NH2 (46) as containing the optimum bridging element (19-membered ring) in this region of the molecule. This analogue (46) was 17 times more potent than the standard.
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360005
06LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
In vitro, the 18-membered ring cyclic analog 51 of hGHRH(1-29)-NH2 was 14 times more potent than the standard.
In plain wordsIn lab tests, a second ring-shaped version of GHRH(1-29) was 14 times more potent than the standard.
Peptide
Sermorelin
Outcome
IncreasePotency of cyclic analog 51
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Measurements
Relative potency
14 times standard
analog 51
Source sentences
Summary
Equally effective was an [i-(i + 3)] constraint yielding the 18-membered ring cyclo(25-28)[MeTyr1,Ala15,Glu25,Nle,27Lys28]- hGHRH-(1-29)-NH2 (51) which was 14 times more potent than the standard.
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360006
07LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
Of 26 lactam-scan analogs in vitro, 11 had less than 10% of the standard's potency, 4 were weak agonists and 4 were equipotent.
In plain wordsIn lab tests, of 26 ring-shaped GHRH(1-29) versions, 11 were much weaker than the standard, 4 were weak and 4 were equal.
Peptide
Sermorelin
Outcome
MixedPotency of Glu-to-Lys lactam scan analogs
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Source sentences
Summary
Of the 26 analogues in the series, 11 had diminished potencies of less than 10% that of the agonist standard, 4 were weak agonists (15-40% relative potency), and 4 analogues were equipotent to the standard.
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360007
08LabNot a test of Sermorelin aloneIn vitro (cells)Activity measurement
The 7 most potent lactam-scan analogs were 3 to 14 times more potent than the standard in vitro.
In plain wordsIn lab tests, the 7 strongest ring-shaped GHRH(1-29) versions were 3 to 14 times more potent than the standard.
Peptide
Sermorelin
Outcome
IncreasePotency of the 7 most potent lactam analogs
Study
n: not reported in source
Comparator
hGHRH(1-40)-OH standard
Outcome group
Receptor activity and mechanism · Endocrine and hormones
Measurements
Relative potency
3 to 14 times standard
7 most potent lactam analogs
Source sentences
Summary
The 7 most potent analogues ranged in potency from 3 to 14 times greater than that of the standard and contained the [i-(i + 3)] cycles between residues 4-7, 5-8, 9-12, 16-19, 21-24, 22-25, and 25-28.
In this study, Sermorelin was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Sermorelin.
Report a problemFND-0951360008

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
10 Oct 2026, 10:21 UTC
Study results updated
Version 1
9 Oct 2026, 03:13 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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