Cabergoline
Overview
Cabergoline an ergot
derivative, is a potent dopamine receptor
agonist
on D2 receptors. In vitro, rat studies show cabergoline has a direct inhibitory effect on pituitary lactotroph
(prolactin
) cells. It is frequently used as a first-line agent in the management of prolactinoma
s due to higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine
.
Cabergoline was invented by scientists working for the Italian drug company Farmitalia-Carlo Erba SpA in Milan
in 1981/82, who were experimenting with semisynthetic derivatives of the ergot
alkaloids.
Ergot
Ergot or ergot fungi refers to a group of fungi of the genus Claviceps. The most prominent member of this group is Claviceps purpurea. This fungus grows on rye and related plants, and produces alkaloids that can cause ergotism in humans and other mammals who consume grains contaminated with its...
derivative, is a potent dopamine receptor
Dopamine receptor
Dopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system . The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors....
agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
on D2 receptors. In vitro, rat studies show cabergoline has a direct inhibitory effect on pituitary lactotroph
Lactotroph
Lactotrophs are cells in the anterior pituitary which produce prolactin in response to signals including dopamine, estrogen, progesterone and Thyrotropin-releasing hormone. Dopamine has an inhibitory effect on PRL secretion...
(prolactin
Prolactin
Prolactin also known as luteotropic hormone is a protein that in humans is encoded by the PRL gene.Prolactin is a peptide hormone discovered by Henry Friesen...
) cells. It is frequently used as a first-line agent in the management of prolactinoma
Prolactinoma
A prolactinoma is a benign tumor of the pituitary gland that produces a hormone called prolactin. It is the most common type of pituitary tumor...
s due to higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine
Bromocriptine
Bromocriptine , an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease , hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.- Indications :Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly...
.
Cabergoline was invented by scientists working for the Italian drug company Farmitalia-Carlo Erba SpA in Milan
Milan
Milan is the second-largest city in Italy and the capital city of the region of Lombardy and of the province of Milan. The city proper has a population of about 1.3 million, while its urban area, roughly coinciding with its administrative province and the bordering Province of Monza and Brianza ,...
in 1981/82, who were experimenting with semisynthetic derivatives of the ergot
Ergot
Ergot or ergot fungi refers to a group of fungi of the genus Claviceps. The most prominent member of this group is Claviceps purpurea. This fungus grows on rye and related plants, and produces alkaloids that can cause ergotism in humans and other mammals who consume grains contaminated with its...
alkaloids.
