Gonadorelin is another name for gonadotropin-releasing hormone (GnRH). It is a synthetic decapeptide prepared using solid phase peptide synthesis. GnRH is responsible for the release of follicle stimulating hormone and leutinizing hormone from the anterior pitutitary. GnRH is available as gonadorelin hydrochloride (Factrel®) and gonadorelin diacetate tetrahydrate(Cystorelin®) for injectable use. Studies have described it being used via an infusion pump system to induce ovulation in patients with hypothalamic hypogonadism. Gonadorelin is a hormone that is produced naturally by the hypothalamus in the brain.  >> Read More

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THE regulation of normal mammalian sexual maturation and reproductive function requires the integration and precise orchestration of hormonal regulation at the hypothalamic, pituitary, and gonadal levels. GnRH is a decapeptide synthesized in neurosecretory cells in the preoptic area of the hypothalamus. GnRH is secreted into the hypophysial portal circulation and is transported to the anterior pituitary gland, where it binds to receptors on a specific pituitary cell type, the gonadotrope, to modulate the synthesis and secretion of the gonadotropins, LH and FSH. Gonadotropins, in turn, are secreted into the systemic circulation and act on the gonads to regulate steroidogenesis and gametogenesis. LH stimulates ovulation and corpus luteum formation in females and androgen secretion in males; FSH stimulates the growth and maturation of ovarian follicles in females and spermatogenesis in males. Gonadal steroids and peptides, in turn, are secreted into the systemic circulation and act to modulate hypothalamic and pituitary function in both positive and negative feedback loops.

Studies of Gonadotropin-Releasing Hormone (GnRH) Action Using nRH Receptor-Expressing Pituitary Cell Lines

Gonadotropin releasing hormone is a hypothalamic decapeptide that stimulates the release of gonadotropic hormones from the anterior pituitary gland. Therapeutically, the human pituitary GnRH receptor is the target of agonists used in the suppression of prostate cancer. Here we report the isolation of a cDNA representing this receptor. It encodes a protein with a transmembrane topology similar with that of other G protein-coupled, 7-transmembrane receptors. Binding studies of the cloned receptor demonstrate high affinity and pharmacological properties similar with the native human pituitary GnRH receptor. Northern blot and reverse transcriptase/PCR analysis revealed that its mRNA is expressed in pituitary, ovary, testis, breast, and prostate but not in liver and spleen. Availability of a human GnRH receptor cDNA should permit the design of improved analogs for therapeutic applications.

Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor