Effects of a sustained release formulation of the gonadotrophin-releasing hormone agonist histrelin on serum concentrations of gonadotrophins and oestradiol, and ovarian LH/human chorionic gonadotrophin receptor content in the rat.

Gunnet JW, Demarest KT, Hahn DW, Ericson E, McGuire JL

The Journal of endocrinology1 Nov 1991Cited by 3 (Europe PMC)

PMID1744568DOI10.1677/joe.0.1310211PepBankPUB-01744568

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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

8 results from studies that gave the peptide. No result from this study comes from people.

01AnimalAnimal study (in vivo)Efficacy outcome
In rats, microencapsulated histrelin caused dose-dependent disruption of oestrous cycles with persistent dioestrous-like vaginal cytology.
In plain wordsIn rats, microencapsulated histrelin disrupted reproductive cycles in a dose-dependent manner.
Peptide
Histrelin
Outcome
DecreaseOestrous cyclicity
Study
ratn: not reported in source
Female rats
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
10-300 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
A single s.c. injection of microencapsulated histrelin (10-300 micrograms peptide/kg) induced a dose-dependent disruption of normal oestrous cyclical activity with a persistent dioestrous-like vaginal cytology.
1 context sentence(design, population, supporting numbers)
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456801
02AnimalAnimal study (in vivo)Efficacy outcome
In rats, serum LH at 1 week was higher with 10 than 300 micrograms/kg microencapsulated histrelin.
In plain wordsIn rats, the lower microencapsulated histrelin dose produced higher LH at 1 week than the higher dose.
Peptide
Histrelin
Outcome
IncreaseLH at one week by dose
Study
ratn: not reported in source
Female rats
Comparator
300 micrograms/kg histrelin
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
10 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
In preliminary studies, pituitary gland stimulation and desensitization were demonstrated when serum LH and FSH levels were greater 1 week after administration of 10 micrograms microencapsulated histrelin/kg compared with 300 micrograms microencapsulated histrelin/kg.
1 context sentence(design, population, supporting numbers)
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456802
03AnimalAnimal study (in vivo)Efficacy outcome
In rats, serum FSH at 1 week was higher with 10 than 300 micrograms/kg microencapsulated histrelin.
In plain wordsIn rats, the lower microencapsulated histrelin dose produced higher FSH at 1 week than the higher dose.
Peptide
Histrelin
Outcome
IncreaseFSH at one week by dose
Study
ratn: not reported in source
Female rats
Comparator
300 micrograms/kg histrelin
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
10 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
In preliminary studies, pituitary gland stimulation and desensitization were demonstrated when serum LH and FSH levels were greater 1 week after administration of 10 micrograms microencapsulated histrelin/kg compared with 300 micrograms microencapsulated histrelin/kg.
1 context sentence(design, population, supporting numbers)
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456803
04AnimalAnimal study (in vivo)Efficacy outcome
In rats receiving microencapsulated histrelin, LH secretion peaked within 8 h, then declined to dioestrous levels from days 7 to 28.
In plain wordsIn rats, microencapsulated histrelin first increased LH, which then declined to dioestrous levels.
Peptide
Histrelin
Outcome
MixedLH secretion over time
Study
ratn: not reported in source
Female rats
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
100 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
LH secretion was maximal within 8 h and then gradually declined, remaining at dioestrous levels from days 7 to 28.
2 context sentences(design, population, supporting numbers)
Summary · context
Changes in pituitary and ovarian function were assessed over time following injection of microencapsulated histrelin (100 micrograms peptide/kg).
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456804
05AnimalAnimal study (in vivo)Efficacy outcome
In rats receiving microencapsulated histrelin, serum oestradiol remained low and rose above dioestrous levels only on day 28.
In plain wordsIn rats receiving microencapsulated histrelin, oestradiol remained low until it rose above dioestrous levels on day 28.
Peptide
Histrelin
Outcome
MixedOestradiol over time
Study
ratn: not reported in source
Female rats
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
100 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
Serum oestradiol concentrations remained low and rose above dioestrous levels only on day 28.
2 context sentences(design, population, supporting numbers)
Summary · context
Changes in pituitary and ovarian function were assessed over time following injection of microencapsulated histrelin (100 micrograms peptide/kg).
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456805
06AnimalAnimal study (in vivo)Mechanism
In rats receiving microencapsulated histrelin, ovarian LH/hCG receptor content fell within 8 h, reached its nadir on day 7, and recovered by day 28.
In plain wordsIn rats receiving microencapsulated histrelin, ovarian LH/hCG receptor content decreased and then recovered by day 28.
Peptide
Histrelin
Outcome
MixedOvarian LH/hCG receptor content
Study
ratn: not reported in source
Female rats
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
100 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
In contrast, ovarian LH/human chorionic gonadotrophin (LH/hCG) receptor content fell within 8 h and, after a nadir on day 7, slowly returned to dioestrous levels by day 28.
2 context sentences(design, population, supporting numbers)
Summary · context
Changes in pituitary and ovarian function were assessed over time following injection of microencapsulated histrelin (100 micrograms peptide/kg).
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456806
07AnimalAnimal study (in vivo)Mechanism
In rats receiving microencapsulated histrelin, ovarian LH/hCG receptor recovery preceded significant changes in pituitary gonadotrophin secretion.
In plain wordsIn rats receiving microencapsulated histrelin, ovarian receptors recovered before pituitary hormone secretion changed significantly.
Peptide
Histrelin
Outcome
Not applicableTiming of ovarian and pituitary recovery
Study
ratn: not reported in source
Female rats
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
100 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
The increase in ovarian LH/hCG receptor content preceded any significant change in pituitary gonadotrophin secretion, indicating a differential pattern of recovery for pituitary and ovarian function.
2 context sentences(design, population, supporting numbers)
Summary · context
Changes in pituitary and ovarian function were assessed over time following injection of microencapsulated histrelin (100 micrograms peptide/kg).
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456807
08AnimalAnimal study (in vivo)Mechanism
In rats, histrelin microcapsules prevented an LH increase after a GnRH challenge 3 days later.
In plain wordsIn rats, microencapsulated histrelin prevented an LH increase after a GnRH challenge.
Peptide
Histrelin
Outcome
DecreaseLH response to GnRH challenge
Study
ratn: not reported in source
Female rats
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
300 micrograms/kg · subcutaneous injectionAs given in this study (rat).
Source sentences
Summary
Treatment with histrelin microcapsules (300 micrograms peptide/kg) prevented any increase in LH secretion in response to a GnRH challenge 3 days later, indicating a direct action of histrelin on the pituitary gland.(ABSTRACT TRUNCATED AT 250 WORDS)
1 context sentence(design, population, supporting numbers)
Summary · context
Pituitary and ovarian function were studied during the loss and recovery of oestrous cyclical activity in rats following treatment with a sustained release formulation of the gonadotrophin-releasing hormone (GnRH) agonist [imidazole benzyl-D-His6,Pro9-ethylamide]-GnRH (histrelin).
Report a problemFND-0174456808

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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
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:35 UTC
First added · source update from Europe PMC

Subjects

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