A dopamine D2 and D3 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 (Request formulation change)
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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    1 mg

    $49

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    5 mg

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    Product Description

    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 D2L and D2S 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.

    References & Product Citations
    Product Description References

    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).