A potent and selective dopamine D2 receptor agonist
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Labeled Version(s)
31690Cabergoline-d6
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Cabergoline

Item No. 23934

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propen-1-yl)-ergoline-8β-carboxamide
CAS Number
81409-90-7
Synonyms
  • FCE 21336
Molecular Formula
C26H37N5O2
Formula Weight
451.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: Slightly SolubleMethanol: Slightly Soluble
SMILES
O=C(NCC)N(CCCN(C)C)C([C@H]1CN(CC=C)[C@@]2([H])[C@](C3=C4C(C2)=CNC4=CC=C3)([H])C1)=O
InChi Code
InChI=1S/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21-,23-/m1/s1
InChi Key
KORNTPPJEAJQIU-KJXAQDMKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Cabergoline is a potent and selective dopamine D2 receptor agonist (Kis = 0.912 and 6,935 nM for D2 and D1 receptors, respectively, in rat striatum) that inhibits the secretion of prolactin (PRL) and growth hormone.1,2 It inhibits PRL secretion in and growth of rat pituitary tumor cells in a concentration-dependent manner, an effect which can be reversed by the dopamine D2 receptor antagonist haloperidol (Item No. 12014).2 Cabergoline suppresses the mammalian target of rapamycin (mTOR) signaling pathway in a time-dependent manner and induces autophagy and cell death in MMQ and GH3 rat pituitary cells.3 In vivo, cabergoline (0.25 mg/kg) stimulates motor activity and decreases dyskinesias in a monkey model of Parkinson's disease induced by MPTP.4 Formulations containing cabergoline have been used to treat prolactinomas.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miyagi, M., Itoh, F., Taya, F., et al. Dopamine receptor affinities in vitro and stereotypic activities in vivo of cabergoline in rats. Biol. 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 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. 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).