General Information of Drug (ID: DM5GKOV)

Drug Name
Pergolide mesylate Drug Info
Synonyms
Pergolida; Pergolide (mesylate); Pergolide Methanesulfonate; Pergolide mesilate; Permax (TN); LY127809; PERGOLIDE MESYLATE; PERGOLIDE MESYLATE SALT; 55B9HQY616; 66104-23-2; 8-beta-((Methylthio)methyl)-6-propylergoline methanesulfonate; 8-beta-((Methylthio)methyl)-6-propylergoline monomethane sulfonate; 8beta-((Methylthio)methyl)-6-propylergoline monomethanesulfonate; CHEBI:8021; CHEMBL1275; CPD000058504; DSSTox_CID_20583; DSSTox_GSID_40583; DSSTox_RID_77029; MLS000069837; MPE; SMR000058504; UNII-55B9HQY616; LY-127,809; LY-127809; Pergolida [INN-Spanish]; Pergolide (INN); Pergolide [INN:BAN]; Pergolidum; Pergolidum [INN-Latin]; Permax; Prestwick0_000295; Prestwick1_000295; Prestwick2_000295; Prestwick3_000295; SR-01000721840; Spectrum2_001970; Spectrum4_000835; Spectrum5_001649; Spectrum_001647; TNP00315; pergolide; (8beta)-8-[(methylsulfanyl)methyl]-6-propylergoline; 24MJ822NZ9; 66104-22-1; CHEBI:63617; CHEMBL531; Ergoline, 8-((methylthio)methyl)-6-propyl-, (8beta)-; NCGC00017366-04; UNII-24MJ822NZ9
Cross-matching ID
PubChem CID
47812
ChEBI ID
CHEBI:8021
CAS Number
CAS 66104-23-2
TTD Drug ID
DM5GKOV
INTEDE Drug ID
DR2412

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial 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 [3]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [4]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [6]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [7]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [8]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [9]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [10]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [4]
Verapamil DMA7PEW Angina pectoris BA40 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By D(2) dopamine receptor (DRD2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Droperidol DM0DXA8 Nausea MD90 Approved [12]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [12]
Zuclopenthixol DMKYD5N Schizophrenia 6A20 Approved [12]
Meglitinides DM1OFHN Type-2 diabetes 5A11 Approved [13]
Sulpiride DMF54ZG Schizophrenia 6A20 Approved [14]
Risperidone DMN6DXL Bipolar I disorder Approved [15]
Olanzapine DMPFN6Y Bipolar depression Approved [16]
Methamphetamine DMPM4SK Anxiety Approved [17]
Bromocriptine DMVE3TK Acromegaly 5A60.0 Approved [18]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By D(1A) dopamine receptor (DRD1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [12]
Haloperidol DM96SE0 Delirium Approved [20]
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [21]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [20]
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [22]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [23]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [24]
Methamphetamine DMPM4SK Anxiety Approved [25]
Clozapine DMFC71L Schizophrenia 6A20 Approved [26]
Bardoxolone methyl DMODA2X Mixed connective tissue disease 4A43.3 Phase 3 [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bepridil DM0RKS4 Chronic/stable angina BA40.1 Approved [28]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [29]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [30]
Decitabine DMQL8XJ Acute myelogenous leukaemia 2A41 Approved [31]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [32]
Carbamazepine DMZOLBI Epilepsy 8A60-8A68 Approved [30]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [33]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [33]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [33]
Ebastine DMH21D9 N. A. N. A. Phase 4 [34]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
D(1A) dopamine receptor (DRD1) OTLZPBT7 DRD1_HUMAN Gene/Protein Processing [2]
D(2) dopamine receptor (DRD2) OTBLXKEG DRD2_HUMAN Gene/Protein Processing [2]
Potassium voltage-gated channel subfamily A member 5 (KCNA5) OTHI2N71 KCNA5_HUMAN Gene/Protein Processing [2]

References

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2 Pergolide is an inhibitor of voltage-gated potassium channels, including Kv1.5, and causes pulmonary vasoconstriction. Circulation. 2005 Sep 6;112(10):1494-9. doi: 10.1161/CIRCULATIONAHA.105.556704. Epub 2005 Aug 29.
3 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.
4 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
5 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.
6 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
7 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.
8 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.
9 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
10 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.
11 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.
12 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
13 Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia. Psychopharmacology (Berl). 2008 Apr;197(2):229-35. doi: 10.1007/s00213-007-1029-z. Epub 2007 Dec 6.
14 Positron emission tomography measurement of dopamine D? receptor occupancy in the pituitary and cerebral cortex: relation to antipsychotic-induced hyperprolactinemia. J Clin Psychiatry. 2010 Sep;71(9):1131-7. doi: 10.4088/JCP.08m04307yel. Epub 2010 Feb 23.
15 Variants of the dopamine D2 receptor gene and risperidone-induced hyperprolactinemia in children and adolescents. Pharmacogenet Genomics. 2009 May;19(5):373-82. doi: 10.1097/FPC.0b013e328329a60f.
16 Dopamine receptor D2 gene is associated with weight gain in schizophrenic patients under long-term atypical antipsychotic treatment. Pharmacogenet Genomics. 2010 Jun;20(6):359-66. doi: 10.1097/FPC.0b013e3283397d06.
17 A preliminary study: novelty seeking, frontal executive function, and dopamine receptor (D2) TaqI A gene polymorphism in patients with methamphetamine dependence. Compr Psychiatry. 2008 Jul-Aug;49(4):387-92. doi: 10.1016/j.comppsych.2008.01.008. Epub 2008 Mar 21.
18 Imaging gene-substance interactions: the effect of the DRD2 TaqIA polymorphism and the dopamine agonist bromocriptine on the brain activation during the anticipation of reward. Neurosci Lett. 2006 Sep 25;405(3):196-201. doi: 10.1016/j.neulet.2006.07.030. Epub 2006 Aug 8.
19 Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. doi: 10.1073/pnas.0609752104. Epub 2007 Jul 2.
20 Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95.
21 Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects. Arch Gen Psychiatry. 1992 Jul;49(7):538-44. doi: 10.1001/archpsyc.1992.01820070032005.
22 Dopamine-mediated inhibition of renal Na+/K+-ATPase in HK-2 cells is reduced by ouabain. Clin Exp Pharmacol Physiol. 2010 May;37(5-6):613-8. doi: 10.1111/j.1440-1681.2010.05364.x. Epub 2010 Feb 4.
23 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.
24 Characterizing fucoxanthin as a selective dopamine D(3)/D(4) receptor agonist: Relevance to Parkinson's disease. Chem Biol Interact. 2019 Sep 1;310:108757. doi: 10.1016/j.cbi.2019.108757. Epub 2019 Jul 16.
25 Dopamine D1 receptor protein is elevated in nucleus accumbens of human, chronic methamphetamine users. Mol Psychiatry. 2000 Nov;5(6):664-72. doi: 10.1038/sj.mp.4000760.
26 Association study of four dopamine D1 receptor gene polymorphisms and clozapine treatment response. J Psychopharmacol. 2007 Sep;21(7):718-27. doi: 10.1177/0269881106072341. Epub 2006 Nov 8.
27 Characterization of the potent, selective Nrf2 activator, 3-(pyridin-3-ylsulfonyl)-5-(trifluoromethyl)-2H-chromen-2-one, in cellular and in vivo models of pulmonary oxidative stress. J Pharmacol Exp Ther. 2017 Oct;363(1):114-125.
28 Inhibitory effect of bepridil on hKv1.5 channel current: comparison with amiodarone and E-4031. Eur J Pharmacol. 2001 Nov 2;430(2-3):149-57. doi: 10.1016/s0014-2999(01)01381-4.
29 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.
30 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
31 Acute hypersensitivity of pluripotent testicular cancer-derived embryonal carcinoma to low-dose 5-aza deoxycytidine is associated with global DNA Damage-associated p53 activation, anti-pluripotency and DNA demethylation. PLoS One. 2012;7(12):e53003. doi: 10.1371/journal.pone.0053003. Epub 2012 Dec 27.
32 Differential effects of estrogen and progesterone on potassium channels expressed in Xenopus oocytes. Steroids. 2008 Mar;73(3):272-9. doi: 10.1016/j.steroids.2007.10.010. Epub 2007 Nov 4.
33 Detection of potassium currents and regulation of multidrug resistance by potassium channels in human gastric cancer cells. Cell Biol Int. 2007 Jul;31(7):741-7. doi: 10.1016/j.cellbi.2007.01.008. Epub 2007 Jan 21.
34 Comparative effects of nonsedating histamine H1 receptor antagonists, ebastine and terfenadine, on human Kv1.5 channels. Eur J Pharmacol. 1997 May 20;326(2-3):257-63. doi: 10.1016/s0014-2999(97)85421-0.