Related Experiment Video
Updated: Aug 30, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Gonadotropin-releasing hormone antagonists
1UCLA School of Medicine, Department of Internal Medicine, Augustus F Hawkins Building, Room 3069, 1731 East 120th Street, Los Angeles, CA 90059, USA. kaherbst@cdrewu.edu
Abstract:
Hypothalamic gonadotropin-releasing hormone (GnRH) is a decapeptide that stimulates pituitary synthesis and secretion of gonadotropins and, therefore, gonadal hormones. GnRH antagonists, of which thousands have been formulated, inhibit the hormone from binding to its receptor, inducing a pharmacological hypophysectomy. Peptide derivations of GnRH and non-peptide compounds are both in clinical trials or approved for assisted reproduction. As these compounds reach the market, the use of antagonists might expand to treatment of other hormonally dependent diseases, hormonal male contraception and growth inhibition of extra-pituitary cancer cells expressing GnRH receptors.
Related Concept Videos
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:

