The effects of depot formulations of the luteinizing hormone-releasing hormone (LHRH) agonist Decapeptyl (25 microg/day) for 30 days or LHRH antagonist Cetrorelix pamoate (100 microg/day) for 30 days and daily injections of 100 microg of Decapeptyl for 10 days on the expression of mRNA for pituitary LHRH receptor (LHRH-R) and the levels of LHRH-R protein were evaluated in rats. Serum sex steroi...

Substitution at positions 6 and 10 can result in super-active peptides. Therefore, several LHRH analogues substituted at position 6, 10, or both are much more active than LHRH and have prolonged activity [5]. Of these analogues, the most important are [D-Trp 6 ]LHRH (triptorelin), [D-Leu 6 ,Pro 9 NHET]LHRH (leuprolide), [D-Ser(Bu t ) 6 ,Pro 9 NHET]LHRH (buserelin), and [D-Ser(Bu t ) 6 ,AzaGly 1...

Mammalian reproduction is dependent upon intermittent delivery of luteinizing hormone-releasing hormone (LHRH) to the anterior pituitary. This mode of secretion is required to sensitize maximally the gonadotrophs to LHRH stimulation and to regulate gonadotropin gene expression. While LHRH secretion is pulsatile in nature, the origin of the pulse generator is unknown. In this report, we show tha...

OBJECTIVE More than 80% of human ovarian cancers express LHRH and its receptor. The proliferation of human ovarian cancer cell lines is reduced by both LHRH agonists and antagonists. This study was designed to further clarify the possible biological function of this LHRH system. DESIGN As LHRH agonists and antagonists uniformly reduce proliferation of human ovarian cancer in a dose-dependent ...

The mechanisms through which luteinizing hormone (LH)-releasing hormone (LHRH) antagonists suppress pituitary gonadotroph functions and LHRH-receptor (LHRH-R) expression are incompletely understood. Consequently, we investigated the direct effect of LHRH antagonist cetrorelix in vitro on the expression of the pituitary LHRH-R gene and its ability to counteract the exogenous LHRH and the agonist...

In the present study, we wished to ascertain if lectin-binding sites are present on hypothalamic granules containing luteinizing hormone-releasing hormone (LHRH). LHRH granules (isolated from homogenates of hypothalami of adult male rats by means of hypo-osmotic shock and differential centrifugation) were subjected to affinity chromatography on columns of concanavalin A (Con A)-Sepharose. The a...

The aim of the present study was to prepare luteinizing-hormone releasing hormone (LHRH) nanoliposomal microbubbles specifically targeting ovarian cancer cells. The lyophilization/sonication method was used to prepare non-targeting nanoliposomal microbubbles (N-N-Mbs). Using the biotin-avidin bridge method, conjugated LHRH antibodies to N-N-Mbs generated LHRH nanoliposomal microbubbles (LHRH-N-...

We and others have identified luteinizing hormone-releasing hormone (LHRH) in cells of the immune system in both animals and humans. LHRH is an immunostimulant, and testosterone is an immunosuppressant. Because testosterone is known to modulate the concentrations of hypothalamic LHRH, we wondered whether testosterone might also alter the concentrations of rat thymic LHRH. Two weeks after castra...

Cytotoxic analogue of luteinizing hormone releasing hormone (LHRH), AN-207, binds with high affinity to LHRH receptors and can be targeted to tumors expressing these receptors. We investigated the expression of LHRH receptors in surgical specimens of human malignant melanoma and evaluated the effects of AN-207 in models of human melanoma. Human melanoma specimens derived from primary tumors or ...