Cabergoline is a D2-like Receptor Agonist for High Prolactin Levels Related Diseases

By Edward Jenner 2023-11-28 #Cabergoline, #Dopamine Receptor, #hyperprolactinemia, #Parkinson's disease

Dopamine Receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling. Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors. There are at least five subtypes of dopamine receptors, D1, D2, D3, D4, and D5. The D1 and D5 receptors are members of the D1-like family of dopamine receptors. And the D2, D3 and D4receptors are members of the D2-like family.

Cabergoline is a D2-like Receptor Agonist for Endocrinology and Cancer

Cabergoline is a D2-like receptor agonist. And it has high affinity for D2, D3, and 5-HT2B receptors with K_i values of 0.7, 1.5, and 1.2 nM, respectively.

In Vitro, Cabergoline acts as a potent agonist of D2, D3 and 5-HT2B receptors. Pretreatment with Cabergoline inhibits H₂O₂-induced neuronal cell death in a dose-dependent manner. To study its neuroprotective effects,10 μM cabergolin is used in the experiment. MAP2 staining reveals that Cabergoline significantly suppresses the loss of neurons caused by H₂O₂ incubation. The detection of apoptotic nuclear condensation suggested that Cabergoline prevents apoptotic cell death following H₂O₂ exposure.

In Vivo, during the light period, the amount of REM sleep in cabergoline-injected restrained males did not differ from vehicle-injected males. However, during the dark phase, restrained men injected with cabergoline spent 46.1% less REM sleep than men injected with vehicle. Cabergoline had no effect on REM sleep in treated male mice. During the light phase and dark phase, the amount of REM sleep in cabergoline-injected men was similar to that in vehicle-injected men.

In conclusion, Cabergoline is a D2-like receptor agonist and has high affinity for D2, D3, and 5-HT2B receptors for Parkinson’s disease and hyperprolactinemia.

Reference:

[1]. PLoS One. 2014 Jun 10;9(6):e99271.

[2]. Endocrinology. 2014 Nov;155(11):4411-21.