Cabergoline-d₆

Cabergoline-d₆ is intended for use as an internal standard for the quantification of cabergoline (Item No. 23934) by GC- or LC-MS. Cabergoline is a dopamine D₂ and D₃ receptor agonist.¹ It inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing a high density of human dopamine D_2L and D_2S receptors (EC₅₀s = 0.0492 and 0.0297 nM, respectively) or dopamine D₃ receptors containing serine or glycine at position 9 (EC₅₀s = 4.41 and 5.1 nM, respectively). Cabergoline inhibits prolactin secretion in primary rat pituitary tumor cells, an effect that can be reversed by haloperidol (Item No. 12014), and suppresses mTOR signaling and induces autophagic cell death in MMQ and GH3 rat pituitary cells.^2,3 It also reduces the development of estrogen-induced prolactinomas in female rats at 0.6 mg/kg.⁴ Cabergoline (5 mg/kg) induces apoptosis of tumor-associated endothelial cells and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of small cell lung cancer (SCLC).⁵ In addition, it stimulates motor activity and induces only transient dyskinesias in a cynomolgus monkey model of Parkinson's disease induced by MPTP when administered at 0.25 mg/kg.⁶ Formulations containing cabergoline have been used in the treatment of hyperprolactinemic disorders, including prolactinomas.

WARNING This product is not for human or veterinary use.

1. Tadori, Y., Forbes, R.A., McQuade, R.D., et al. Functional potencies of dopamine agonists and antagonists at human dopamine D₂ and D₃ receptors. Eur. J. Pharmacol. 666(1-3), 43-52 (2011).

2. Eguchi, K., Kawamoto, K., Uozumi, T., et al. Effect of cabergoline, a dopamine agonist, on estrogen-induced rat pituitary tumors: In vitro culture studies. Endocr. J. 42(3), 413-420 (1995).

3. Lin, S.J., Leng, Z.G., Guo, Y.H., et al. Suppression of mTOR pathway and induction of autophagy-dependent cell death by cabergoline. Oncotarget 6(36), 39329-39341 (2015).

4. Dall'Ara, A., Lima, L., Cocchi, D., et al. Inhibitory effect of cabergoline on the development of estrogen-induced prolactin-secreting adenomas of the pituitary. Eur. J. Pharmacol. 151(1), 97-102 (1988).

5. Alam, S.K., Pandit, A., Wang, L., et al. Dopamine D₂ receptor agonists abrogate neuroendocrine tumour angiogenesis to inhibit chemotherapy-refractory small cell lung cancer progression. Cell Death Dis. 16(1), 370 (2025).

6. Grondin, R., Goulet, M.T., Di Paolo, T., et al. Cabergoline, a long-acting dopamine D₂-like receptor agonist, produces a sustained antiparkinsonian effect with transient dyskinesias in parkinsonian drug-naive primates. Brain Res. 735(2), 298-306 (1996).