General Information of Drug (ID: DM1EF73)

Drug Name
Methysergide Drug Info
Synonyms
Deseril; Desernil; Desernyl; Deseryl; Desril; Dimethylergometrin; Methylmethylergonovine; Methysergid; Methysergidum; Metisergide; Metisergido; Sansert; Methyllysergic acid butanolamide; Metisergide [DCIT]; UML 491; Deseril (TN); Methysergidum [INN-Latin]; Metisergido [INN-Spanish]; Sansert (TN); UML-491; Methysergide (USAN/INN); Methysergide [USAN:INN:BAN]; N-(alpha-(Hydroxymethyl)propyl)-1-methyl-dextro-lysergamide; N-(1-(Hydroxymethyl)propyl)-1-methyl-dextro-(+)-lysergamide; (+)-9,10-Didehydro-N-(1-(hydroxymethyl)propyl)-1,6-dimethylergoline-8beta-carboxamide; (+)-N-(1-(Hydroxymethyl)propyl)-1-methyl-D-lysergamide; (8beta)-N-[(1S)-1-(hydroxymethyl)propyl]-1,6-dimethyl-9,10-didehydroergoline-8-carboxamide; 1-Methyl-D-lysergic acid butanolamide; 1-Methyl-dextro-lysergic acid (+)-1-hydroxy-2-butylamide; 1-Methylmethylergonovine; 9,10-Didehydro-N-(1-(hydroxymethyl)propyl)-1,6-dimethylergoline-8-carboxamide
Indication
Disease Entry ICD 11 Status REF
Migraine 8A80 Approved [1]
Therapeutic Class
Vasoconstrictor Agents
Cross-matching ID
PubChem CID
9681
ChEBI ID
CHEBI:92629
CAS Number
CAS 361-37-5
TTD Drug ID
DM1EF73
VARIDT Drug ID
DR01419

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting 5-HT 2C receptor (HTR2C)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [5]
Lorcaserin DMG6OYJ Obesity 5B81 Approved [6]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [7]
Mirtazapine DML53ZJ Depression 6A70-6A7Z Approved [8]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [9]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [10]
M100907 DM7ZFBA Sleep-wake disorder 7A00-7B2Z Phase 3 [11]
SR46349B DM1ODMR Primary insomnia 7A00 Phase 3 [12]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [13]
Nuplazid DMOJA5G Alzheimer disease 8A20 Phase 2 [14]
⏷ 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 [15]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [16]
Methotrexate DM2TEOL Anterior urethra cancer Approved [17]
Folic Acid DMEMBJC Colorectal carcinoma Approved [18]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [17]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [17]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [17]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [24]
Methotrexate DM2TEOL Anterior urethra cancer Approved [25]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [4]
Quercetin DM3NC4M Obesity 5B81 Approved [26]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [27]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [28]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [29]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [30]
⏷ 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
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Antagonist [2]

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

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Gene/Protein Processing [4]

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: 134).
2 Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8.
3 Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37.
4 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
5 Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
6 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
7 The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
8 Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulatio... Mol Pharmacol. 2008 Mar;73(3):748-57.
9 Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60.
10 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
11 Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
12 SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 2002 Sep;27(3):430-41.
13 Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
14 The neuropharmacology of sleep paralysis hallucinations: serotonin 2A activation and a novel therapeutic drug. Psychopharmacology (Berl). 2018 Nov;235(11):3083-3091.
15 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
16 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
17 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.
18 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
19 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
20 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
21 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.
22 [Reversal effect of MDR1 and MDR3 gene silencing on resistance of A2780/taxol cells to paclitaxel]. Zhonghua Fu Chan Ke Za Zhi. 2007 Jun;42(6):412-6.
23 8-Methoxypsoralen disrupts MDR3-mediated phospholipids efflux and bile acid homeostasis and its relevance to hepatotoxicity. Toxicology. 2017 Jul 1;386:40-48. doi: 10.1016/j.tox.2017.05.011. Epub 2017 May 24.
24 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
25 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
26 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
27 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
28 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
29 Evaluation of gene induction of drug-metabolizing enzymes and transporters in primary culture of human hepatocytes using high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi. 2002 May;122(5):339-61.
30 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.