Cabergoline-d6 is intended for use as an internal standard for the quantification of cabergoline by GC- or LC-MS. Cabergoline is a dopamine D2 receptor agonist (Ki = 0.912 nM in rat striatal homogenates).1 It is selective for dopamine D2 over D1 receptors (Ki = 6,935 nM). Cabergoline inhibits prolactin secretion in, and growth of, isolated rat pituitary tumor cells in a concentration-dependent manner, an effect that can be blocked by the dopamine D2 receptor antagonist haloperidol .2 Cabergoline reduces phosphorylation of mammalian target of rapamycin (mTOR) and induces the formation of LC3 puncta, a marker of autophagy, and apoptosis in MMQ rat pituitary cells.3 In vivo, cabergoline (0.25 mg/kg) stimulates motor activity and decreases dyskinesias in a cynomolgus monkey model of Parkinson's disease induced by MPTP.4 Formulations containing cabergoline have been used in the treatment of prolactinomas.
1.Miyagi, M., Itoh, F., Taya, F., et al.Dopamine receptor affinities in vitro and stereotypic activities in vivo of cabergoline in ratsBiol. Pharm. Bull.19(9)1210-1213(1996) 2.Eguchi, K., Kawamoto, K., Uozumi, T., et al.Effect of cabergoline, a dopamine agonist, on estrogen-induced rat pituitary tumors: In vitro culture studiesEndocr. 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 cabergolineOncotarget6(36)39329-39341(2015) 4.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 primatesBrain Res.735(2)298-306(1996)