Caberos (Cabergoline)

About the Product

Caberos is a research compound from Driada Medical, containing Cabergoline. Cabergoline is a potent, long-acting dopamine receptor agonist with high affinity for the D2-like receptor family (D2R) . Its molecular formula is C₂₆H₃₇N₅O₂, with a molecular weight of 451.6 g/mol. It is a synthetic ergoline derivative, structurally related to other ergot alkaloids .

The compound functions primarily as a D2-like receptor agonist, acting similarly to endogenous dopamine. This mechanism has made it a standard tool for research into the hypothalamic-pituitary-gonadal (HPG) axis and metabolic regulation . Cabergoline’s long half-life allows for intermittent dosing in research models, distinguishing it from other dopamine agonists .

The product is intended for laboratory research use only and features an integrated QR code on the packaging for detailed product verification.

• Product Name: Caberos (Cabergoline)

• Brand: Driada Medical

• Form: Solution for research applications

• CAS Number: 81409-90-7

• For Research Use Only.

Research Applications & Mechanism of Action

• Potent D2-like Receptor Agonist: Cabergoline functions as a potent agonist at dopamine D2-like receptors (D2R, D3R, D4R) . This binding activates inhibitory G-protein coupled signaling cascades, leading to decreased production of cyclic AMP and subsequent inhibition of target cell function .

• Endocrine & Reproductive Research: Cabergoline is a benchmark compound for studying the HPG axis, particularly in models of hyperprolactinemia and prolactinomas. By activating D2R on pituitary lactotroph cells, cabergoline potently suppresses prolactin (PRL) secretion and reduces lactotroph cell proliferation . Its ability to normalize prolactin levels and restore fertility makes it a key tool in reproductive endocrinology and developmental programming studies .

• Metabolic Research: Cabergoline has demonstrated significant effects on body composition, energy balance, and lipid metabolism . Research applications include studying its role in reducing visceral adiposity, improving insulin sensitivity, and modulating lipid accumulation in both adipocytes and myocytes .

• Neuroscience & Neuroprotection: Emerging research has highlighted cabergoline's potential neuroprotective and cognitive-enhancing properties . Studies demonstrate that cabergoline can ameliorate cognitive decline, reduce neuroinflammation, and enhance autophagic clearance of pathological protein aggregates (Aβ42 and p-tau) in Alzheimer's disease models, primarily through modulation of AKT/mTOR and GLT-1/P38-MAPK signaling pathways . This positions cabergoline as a compound of interest in drug repurposing studies for neurodegenerative conditions .

• Receptor Binding Studies: Cabergoline is also used to study dopamine receptor binding dynamics and signaling selectivity. Its interaction with 5-HT2A and 5-HT2B serotonin receptors is of particular research interest, as this cross-reactivity is associated with the risk of fibrotic valvular heart disease (VHD) . Studies have demonstrated that the bulky N(6) allyl substituent of cabergoline is responsible for its agonism at these serotonin receptors, providing a molecular basis for structure-activity relationship (SAR) studies .

Research & Scientific Background

• Mechanism: Cabergoline’s primary mechanism is D2R agonism. In the pituitary, this inhibits prolactin release; in peripheral tissues, it influences metabolism through mechanisms involving central and peripheral targets, including the endocrine pancreas, adipose tissue, and skeletal muscle . Chronic administration has been shown to positively impact insulin secretion and sensitivity . It has also been shown to induce autophagy, which may be relevant for clearing intracellular aggregates .

• Receptor Selectivity: Cabergoline is not entirely selective for dopamine receptors. Research has shown that its bulky N(6) substituent also enables agonism at 5-HT2A and 5-HT2B serotonin receptors . This is a critical area of investigation, as agonism at 5-HT2B is linked to valvular heart disease . The drug's profile at native serotonin receptors suggests these may not be the primary driver of VHD in vivo, but the interaction remains a significant research consideration .

• Pharmacogenomics: Inter-individual variability in cabergoline response is a growing area of research. Genetic factors influencing the dose-response relationship have been identified. For instance, in a prospective study of 310 prolactinoma patients, dose-response curves demonstrated that effective weekly doses varied significantly based on patient history and tumor characteristics (e.g., ED50 of 0.66 mg/week for bromocriptine-intolerant patients, 1.36 mg/week for naïve patients, and 3.30 mg/week for bromocriptine-resistant patients) . This indicates a clear potential for genetic and phenotypic factors to influence treatment sensitivity.