Effects of long-acting GnRH antagonist, degarelix acetate, on plasma insulin-like peptide 3, testosterone and luteinizing hormone concentrations, and scrotal circumference in male goats

Hannan, M.A.; Kawate, Noritoshi; Fukami, Y.; Weerakoon, W.W.P.N.; Büllesbach, Erika E.; Inaba, Toshio; Tamada, Hiromichi

doi:10.1016/j.theriogenology.2016.09.032

Cited by 11 publications

(20 citation statements)

References 29 publications

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“…In men with prostate cancer, monthly treatments with degarelix acetate for 12 months were reported to achieve a 90% reduction in plasma testosterone concentrations throughout the treatment period compared to the pretreatment value [11]. Our current study confirmed the previous findings in goats that plasma testosterone concentrations immediately declined after degarelix acetate treatment and INSL3 also decreased within a few days after the treatment [10], suggesting that these two testicular hormones are regulated by different mechanisms.…”

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confidence: 88%

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Inhibitory effects of long-term repeated treatments of a sustainable GnRH antagonist, degarelix acetate, on caprine testicular functions

Kawate

Kanuki

Hannan

et al. 2020

Journal of Reproduction and Development

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We investigated the effects of long-term repeated treatments with a sustainable gonadotropin-releasing hormone (GnRH) antagonist, degarelix acetate, on testicular hormonal secretion, size, ultrasound images, histology and spermatogenesis in goats to assess its efficacy as a chemical castration method. Male Shiba goats (3-6 months of age) were treated subcutaneously with degarelix acetate every 4 weeks for 24 weeks. Plasma testosterone and insulin-like peptide 3 (INSL3) concentrations decreased (P<0.05) within 2 days after the first treatment and remained low until 29 weeks (P<0.05). Scrotal circumference and testicular pixel intensity were lower from 2-6 months and from 1-6 months, respectively, compared to the pretreatment values (P<0.05). The testis and epididymis weights were lower at 24 weeks compared to those in untreated goats (P<0.05). There were no sperm in the seminiferous tubules of testicular tissue sections or in homogenates of the epididymis at 24 weeks. These results suggest that repeated treatment with degarelix acetate is an effective chemical castration method for goats.

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confidence: 88%

“…We have reported previously that after a single injection of degarelix acetate in goats, the blood concentrations of insulin-like peptide 3 (INSL3) and testosterone were reduced significantly for two months, followed by a recovery to basal level [10].…”

mentioning

confidence: 99%

Inhibitory effects of long-term repeated treatments of a sustainable GnRH antagonist, degarelix acetate, on caprine testicular functions

Kawate

Kanuki

Hannan

et al. 2020

Journal of Reproduction and Development

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“…In this context, it was previously demonstrated that scrotal circumference showed a higher correlation with plasma INSL3 than with testosterone concentrations during puberty and post-puberty [ 13 ]. INSL3 is secreted in pulses into circulating blood in bulls and bucks in response to luteinizing hormone (LH), but the amplitude of INSL3 pulses is much lower than that of testosterone [ 13 , 27 , 28 , 29 ]; this suggests that INSL3 may be a more stable marker than testosterone for single time point blood sample measurements for the evaluation of total Leydig cell count per pair of testes. It is unclear why the correlation coefficient value was lower for inhibin concentrations with the scrotal circumferences than INSL3 and testosterone; however, it could be related to the formation of the blood-testicular barrier which restricts the immediate release of inhibin from Sertoli cells to circulating blood during development [ 33 ].…”

Section: Discussionmentioning

confidence: 99%

“…Plasma INSL3 concentrations increased continuously from birth to pre-puberty, while testosterone concentrations increased only in the latter phase in Japanese Black beef bull calves, suggesting differential regulation of the two hormonal secretions from testicular Leydig cells in ruminants [ 27 , 28 , 29 ]. In this study, plasma testosterone concentrations did not increase significantly from 0 to 3 months but rose significantly during the same period in the Japanese Black beef bull calves in the previous study [ 11 ].…”

Section: Discussionmentioning

confidence: 99%

Relationships of plasma insulin-like peptide 3, testosterone, inhibin, and insulin-like growth factor-I concentrations with scrotal circumference and testicular weight in Japanese Black beef bull calves

Sakase

Kitagawa

Kibushi

et al. 2018

Journal of Reproduction and Development

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This study was conducted to clarify the relationships of plasma concentrations of insulin-like peptide 3 (INSL3), testosterone, inhibin, and insulin-like growth factor-I (IGF-I) with scrotal circumference and testicular weight in Japanese Black beef bull calves (n = 20), from birth to pre-puberty. Monthly blood sampling (0 to 7 months) and scrotal circumference measurements (0 to 7 months) were performed. Testicular weight was recorded immediately after castration at 7 months. Plasma INSL3, testosterone, inhibin, and IGF-I concentrations were measured either by enzyme immunoassay or time-resolved fluorescence immunoassay. The correlation coefficients of these hormonal concentrations with scrotal circumference were significant (P < 0.0001) and it was higher for INSL3 (r = 0.647) than for testosterone (r = 0.597), IGF-I (r = 0.400), and inhibin (r = –0.453). Calves with heavier testes (> 60 g) at castration (7 months) had higher (P < 0.05) plasma INSL3 (from 3 to 7 months) and inhibin (from 1 to 4 months) concentrations than those with lighter testes (< 60 g). The calves with heavier testes at castration had larger (P < 0.05) scrotal circumference than those with lighter testes from 3 to 7 months. In conclusion, blood INSL3 concentrations may be the best functional indicator among the hormones analyzed for determining total testicular volume during pre-puberty in bull calves. In addition, inhibin and INSL3 concentrations in early calfhood may be functional predictors for testicular weight at pre-puberty.

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“…The initial models for the receptor were based on the crystal structures of human and Cα [Pro 7.45(316) ] ( Figure S1B) in contrast to the other models that represent helix 11 TM7 with no kink at its lower portion ( Figure S1A). Thus, the model based on the 3dqb does not offer a good representation for the conformation of the particular helix.…”

Section: Iii1 Homology Modelmentioning

confidence: 99%

Refinement of the gonadotropin releasing hormone receptor I homology model by applying molecular dynamics

Tzoupis

Nteli

Platts

et al. 2019

Journal of Molecular Graphics and Modelling

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Sexual maturation of human cells in ovaries and prostate is linked to the biochemical cascade initiated by the activation of cell receptors through the binding of Gonadotropin Releasing Hormone (GnRH). The GnRH receptors (GnRHR) are part of the rhodopsin G-protein-coupled receptor (GPCR) family and consist of seven trans-membrane helical domains connected via extra-and intra-cellular segments. The GnRH-GnRHR complex has been implicated in various forms of prostate and ovarian cancer. The lack of any structural data about the GnRH receptor impedes the design of antagonists for use in cancer treatment. The aim of the study is to devise a model of GnRHR to be used further for the design of improved peptide / non-peptide GnRH analogues and, to our knowledge provide new structural information regarding the extracellular loop 2 (ECL2) that acts a regulator of ligand entry to GnRHR. The common structural characteristics, of the members of the rhodopsin family of GPCRs, have been employed for the construction of a homology model for GnRHR. Structural information from the human β2-adrenergic receptor, as well as rhodopsins have been used in order to create a theoretical model for GnRHR. Furthermore, molecular dynamics (MD) simulations have been employed for the refinement of the model and to explore the impact of the bilayer membrane in GnRHR conformation.

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Effects of long-acting GnRH antagonist, degarelix acetate, on plasma insulin-like peptide 3, testosterone and luteinizing hormone concentrations, and scrotal circumference in male goats

Cited by 11 publications

References 29 publications

Inhibitory effects of long-term repeated treatments of a sustainable GnRH antagonist, degarelix acetate, on caprine testicular functions

Inhibitory effects of long-term repeated treatments of a sustainable GnRH antagonist, degarelix acetate, on caprine testicular functions

Relationships of plasma insulin-like peptide 3, testosterone, inhibin, and insulin-like growth factor-I concentrations with scrotal circumference and testicular weight in Japanese Black beef bull calves

Refinement of the gonadotropin releasing hormone receptor I homology model by applying molecular dynamics

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