What is the Origin of GnRHR?

The term originates from the foundational discoveries in neuroendocrinology that elucidated the hypothalamic-pituitary-gonadal (HPG) axis, the system governing reproduction. The receptor's structure and function were characterized following the isolation and sequencing of GnRH itself. Its pharmacological manipulation is central to treatments for infertility, prostate cancer, and precocious puberty.

What is the Mechanism of GnRHR?

Upon binding to GnRH, the GnRHR activates an intracellular signaling cascade, primarily involving the phosphatidylinositol-calcium second messenger system. This activation ultimately stimulates the synthesis and pulsatile release of the gonadotropins, Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH). Prolonged, non-pulsatile activation of the GnRHR leads to desensitization and downregulation, a therapeutic strategy utilized to suppress sex hormone production in certain clinical conditions.

GnRHR

Meaning

Gonadotropin-Releasing Hormone Receptor, a specific G protein-coupled receptor (GPCR) predominantly expressed on the gonadotrope cells of the anterior pituitary gland. This receptor is the critical mediator for the effects of Gonadotropin-Releasing Hormone (GnRH), a decapeptide hormone released in a pulsatile fashion from the hypothalamus. The binding of GnRH to GnRHR is the master switch for the reproductive endocrine axis. GnRHR is also found in extrapituitary tissues like the ovary and prostate.