2001
DOI: 10.1016/s1472-6483(10)62236-5
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The role of LHRH agonists and antagonists

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Cited by 32 publications
(16 citation statements)
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“…This phenomenon has been attributed to downregulation of the GnRH receptors combined with disruption of the postreceptor signaling process (3)(4)(5). Gonadotropin-releasing hormone agonists have been used extensively in controlled ovarian hyperstimulation protocols for IVF to prevent premature luteinization.…”
Section: Discussionmentioning
confidence: 99%
“…This phenomenon has been attributed to downregulation of the GnRH receptors combined with disruption of the postreceptor signaling process (3)(4)(5). Gonadotropin-releasing hormone agonists have been used extensively in controlled ovarian hyperstimulation protocols for IVF to prevent premature luteinization.…”
Section: Discussionmentioning
confidence: 99%
“…After their binding to the receptors, they initially cause gonadotropin release (flare-up effect), and after several days of continuous administration they result in a dramatic drop of the circulating concentrations of FSH and LH through a desensitization mechanism. GnRH agonists have greater affinity for the GnRHR than native GnRH; they also have greater resistance to enzymatic breakdown and a prolonged half-life compared to native GnRH (i.e., native GnRH has a half-life of about 2-4 min compared to 3 h for GnRH agonist, leuprolide) [40]. The internalization of receptors and the slow dissociation of the agonist-receptor complex decrease the total number of functional GnRHRs, leading to a prolonged desensitization [41].…”
Section: Gnrh Agonistsmentioning
confidence: 99%
“…Currently, at least five antagonists are in clinical studies; however, they are mainly for assisted reproduction and cancer treatment (abarelix, antarelix cetrolelix, degarelix and ganirelix) [19][20][21][22][23][24][25][26][27]. Cetrorelix is the most studied antagonist so far.…”
Section: Gnrh Antagonistsmentioning
confidence: 99%
“…The GnRH antagonists seem to have some advantages in assisted reproduction with fewer adverse effects but have 497 somewhat lower pregnancy rates [21]. A randomised, controlled study [21,27] on controlled ovulation has compared cetrorelix with buserelin but no significant differences of importance were demonstrated.…”
Section: Gnrh Antagonistsmentioning
confidence: 99%
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