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Non-ergoline dopamine receptor agonists have higher binding affinity to dopamine D 3-receptors than dopamine D 2-receptors. This binding affinity is related to D 2 and D 3 receptor homology, the homology between them has a high degree of sequence and is closest in their transmembrane domains, were they share around 75% of the amino acid.
Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels). [1] Agonists of the dopamine D 2 receptor such as bromocriptine and cabergoline are able to strongly suppress pituitary prolactin secretion and thereby decrease circulating prolactin levels, and so are most commonly used as prolactin inhibitors. [1]
Dopamine is also synthesized in plants and most animals. In the brain, dopamine functions as a neurotransmitter—a chemical released by neurons (nerve cells) to send signals to other nerve cells. Neurotransmitters are synthesized in specific regions of the brain but affect many regions systemically.
Prolactin (PRL), also known as lactotropin and mammotropin, is a protein best known for its role in enabling mammals to produce milk. It is influential in over 300 separate processes in various vertebrates, including humans. [5] Prolactin is secreted from the pituitary gland in response to eating, mating, estrogen treatment, ovulation and ...
Dopamine agonists are currently the most common methods used for treating hyperprolactinemia. However, since dopamine agonists only negatively regulate prolactin production from the pituitary gland, a few studies have tried to develop prolactin receptor antagonists for potentially treating the dopamine-resistant local hyperprolactinemia.
A prolactin cell (also known as a lactotropic cell, epsilon acidophil, lactotrope, lactotroph, mammatroph, mammotroph) is a cell in the anterior pituitary which produces prolactin (a peptide hormone) in response to hormonal signals including dopamine (which is inhibitory), thyrotropin-releasing hormone and estrogen (especially during pregnancy), which are stimulatory.
Bromocriptine, originally marketed as Parlodel and subsequently under many brand names, [1] is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease, hyperprolactinaemia, neuroleptic malignant syndrome, and, as an adjunct, type 2 diabetes.
Cabergoline, sold under the brand name Dostinex among others, is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson's disease, and for other indications. [2] It is taken by mouth. Cabergoline is an ergot derivative and a potent dopamine D 2 receptor agonist. [3]