| 包装: | 1mg |
| 规格: | 98% |
| 市场价: | 17781元 |
| 分子量: | 457.6 |
Background:
Cabergoline-d6is intended for use as an internal standard for the quantification of cabergoline by GC- or LC-MS. Cabergoline is a dopamine D2receptor agonist (Ki= 0.912 nM in rat striatal homogenates).1It is selective for dopamine D2over D1receptors (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 D2receptor antagonist haloperidol .2Cabergoline 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.3In vivo, cabergoline (0.25 mg/kg) stimulates motor activity and decreases dyskinesias in a cynomolgus monkey model of Parkinson's disease induced by MPTP.4Formulations 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)
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