General Information of Drug (ID: DMQ4HIN)

Drug Name
Cabergoline Drug Info
Synonyms
Cabaser; Cabaseril; Cabergolina; Cabergolinum; Dostinex; Galastop; Sogilen; Cabergolina [Spanish]; Cabergolinum [Latin]; CG-101; Cabaser (TN); Dostinex (TN); FCE-21336; Cabergoline [USAN:BAN:INN]; Cabergoline (JAN/USAN/INN); (8R)-6-allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide; (8beta)-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)-6-(prop-2-en-1-yl)ergoline-8-carboxamide; (8beta)-N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide; (8beta)-N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-prop-2-en-1-ylergoline-8-carboxamide; 1-((6-Allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea; 1-[(6-allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea; 1-ethyl-2-(3'-dimethylaminopropyl)-3-(6'-allylergoline-8'-beta-carbonyl)urea diphosphate; 1-ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea
Indication
Disease Entry ICD 11 Status REF
Hyperprolactinaemia 5A60.1 Approved [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
54746
ChEBI ID
CHEBI:3286
CAS Number
CAS 81409-90-7
TTD Drug ID
DMQ4HIN
VARIDT Drug ID
DR00069
INTEDE Drug ID
DR0253
ACDINA Drug ID
D00086

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [7]
Haloperidol DM96SE0 Delirium Approved [8]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [9]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [10]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [11]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [12]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [13]
Pimozide DMW83TP Schizophrenia 6A20 Approved [14]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [15]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [16]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [17]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [18]
Methotrexate DM2TEOL Anterior urethra cancer Approved [19]
Folic Acid DMEMBJC Colorectal carcinoma Approved [20]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [19]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [19]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [19]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [22]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [25]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [26]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [27]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [30]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [31]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Prolactin (PRL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [33]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [34]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [35]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [36]
Methotrexate DM2TEOL Anterior urethra cancer Approved [37]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [38]
Naloxone DM3FXMA Narcotic depression 6A7Z Approved [39]
Aripiprazole DM3NUMH Bipolar I disorder Approved [40]
Fluoxetine DM3PD2C Bipolar depression Approved [41]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aspirin DM672AH Acute coronary syndrome BA41 Approved [43]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [44]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [45]
Selenium DM25CGV N. A. N. A. Approved [46]
Methotrexate DM2TEOL Anterior urethra cancer Approved [47]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [48]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [49]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [49]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [50]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [51]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Haloperidol DM96SE0 Delirium Approved [52]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [53]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [54]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [55]
Bupivacaine DM4PRFC Anaesthesia 9A78.6 Approved [56]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [57]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [58]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [59]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [60]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [61]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Agonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Brain-derived neurotrophic factor (BDNF) OTLGH7EW BDNF_HUMAN Gene/Protein Processing [5]
Cyclic AMP-responsive element-binding protein 1 (CREB1) OT1MDLA1 CREB1_HUMAN Gene/Protein Processing [5]
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Gene/Protein Processing [6]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 37).
2 Role of D1 and D2 receptors in the regulation of voluntary movements. Bull Exp Biol Med. 2008 Jul;146(1):14-7.
3 Polymorphisms of the drug transporter gene ABCB1 predict side effects of treatment with cabergoline in patients with PRL adenomas. Eur J Endocrinol. 2012 Sep;167(3):327-35.
4 Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67.
5 Atractylon, a novel dopamine 2 receptor agonist, ameliorates Parkinsonian like motor dysfunctions in MPTP-induced mice. Neurotoxicology. 2022 Mar;89:121-126. doi: 10.1016/j.neuro.2022.01.010. Epub 2022 Jan 31.
6 Massive reduction of tumour load and normalisation of hyperprolactinaemia after high dose cabergoline in metastasised prolactinoma causing thoracic syringomyelia. J Neurol Neurosurg Psychiatry. 2004 Oct;75(10):1489-91. doi: 10.1136/jnnp.2003.028118.
7 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
8 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
9 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
10 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
11 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
12 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3639).
13 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
14 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
15 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
16 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
17 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
18 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
19 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
20 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
21 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
22 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
23 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
24 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
25 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
26 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
27 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
28 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
29 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
30 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
31 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
32 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
33 Verapamil-induced hyperprolactinemia complicated by a pituitary incidentaloma. Ann Pharmacother. 1995 Oct;29(10):999-1001. doi: 10.1177/106002809502901009.
34 [Impotence and gynecomastia secondary to hyperprolactinemia induced by ranitidine]. Therapie. 1994 Jul-Aug;49(4):361-2.
35 Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol. 2005 Jul 15;239(1-2):27-36. doi: 10.1016/j.mce.2005.04.008.
36 Cholinergic modulation of the cerebral metabolic response to citalopram in Alzheimer's disease. Brain. 2009 Feb;132(Pt 2):392-401. doi: 10.1093/brain/awn326. Epub 2009 Jan 19.
37 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
38 The effect of thioridazine on prolactinoma growth in a schizophrenic man: case report. Gen Hosp Psychiatry. 1985 Oct;7(4):364-6. doi: 10.1016/0163-8343(85)90053-2.
39 Influence of naloxone on muscle sympathetic nerve activity, systemic and calf haemodynamics and ambulatory blood pressure after exercise in mild essential hypertension. J Hypertens. 1995 Apr;13(4):447-61.
40 The efficacy, safety, and tolerability of aripiprazole for the treatment of schizoaffective disorder: results from a pooled analysis of a sub-population of subjects from two randomized, double-blind, placebo-controlled, pivotal trials. J Affect Disord. 2009 May;115(1-2):18-26. doi: 10.1016/j.jad.2008.12.017. Epub 2009 Feb 23.
41 Serum prolactin levels among outpatients with major depressive disorder during the acute phase of treatment with fluoxetine. J Clin Psychiatry. 2006 Jun;67(6):952-7. doi: 10.4088/jcp.v67n0612.
42 Massive breast enlargement in a patient receiving D-penicillamine for systemic sclerosis. J Rheumatol. 1985 Oct;12(5):990-1.
43 Association between treatment-emergent suicidal ideation with citalopram and polymorphisms near cyclic adenosine monophosphate response element binding protein in the STAR*D study. Arch Gen Psychiatry. 2007 Jun;64(6):689-97. doi: 10.1001/archpsyc.64.6.689.
44 Cannabidiol upregulates melanogenesis through CB1 dependent pathway by activating p38 MAPK and p42/44 MAPK. Chem Biol Interact. 2017 Aug 1;273:107-114. doi: 10.1016/j.cbi.2017.06.005. Epub 2017 Jun 7.
45 Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802.
46 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
47 Distinct genetic profile in peripheral blood mononuclear cells of psoriatic arthritis patients treated with methotrexate and TNF-inhibitors. Clin Rheumatol. 2014 Dec;33(12):1815-21. doi: 10.1007/s10067-014-2807-8. Epub 2014 Oct 24.
48 Peroxisome proliferator-activated receptor-gamma ligands suppress fibronectin gene expression in human lung carcinoma cells: involvement of both CRE and Sp1. Am J Physiol Lung Cell Mol Physiol. 2005 Sep;289(3):L419-28. doi: 10.1152/ajplung.00002.2005. Epub 2005 May 20.
49 Nonclassical action of retinoic acid on the activation of the cAMP response element-binding protein in normal human bronchial epithelial cells. Mol Biol Cell. 2006 Feb;17(2):566-75. doi: 10.1091/mbc.e05-06-0519. Epub 2005 Nov 9.
50 p38 MAPK/PP2Ac/TTP pathway on the connection of TNF- and caspases activation on hydroquinone-induced apoptosis. Carcinogenesis. 2013 Apr;34(4):818-27. doi: 10.1093/carcin/bgs409. Epub 2013 Jan 3.
51 Glycyrrhizin attenuates histamine-mediated MUC5AC upregulation, inflammatory cytokine production, and aquaporin 5 downregulation through suppressing the NF-B pathway in human nasal epithelial cells. Chem Biol Interact. 2018 Apr 1;285:21-26. doi: 10.1016/j.cbi.2018.02.010. Epub 2018 Feb 13.
52 The differential effects of neuroleptic drugs and PACAP on the expression of BDNF mRNA and protein in a human glioblastoma cell line. Acta Neurobiol Exp (Wars). 2017;77(3):205-213.
53 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
54 Tea polyphenols ameliorates neural redox imbalance and mitochondrial dysfunction via mechanisms linking the key circadian regular Bmal1. Food Chem Toxicol. 2017 Dec;110:189-199. doi: 10.1016/j.fct.2017.10.031. Epub 2017 Oct 20.
55 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
56 LncRNA SNHG12 ameliorates bupivacaine-induced neurotoxicity by sponging miR-497-5p to upregulate NLRX1. Hum Exp Toxicol. 2022 Jan-Dec;41:9603271221089001. doi: 10.1177/09603271221089001.
57 Mechanism of arsenic trioxide inhibiting angiogenesis in multiple myeloma. J Huazhong Univ Sci Technolog Med Sci. 2006;26(1):43-6. doi: 10.1007/BF02828035.
58 THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
59 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
60 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
61 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.