Metisergid (UML-491, Sansert, Deseril) je lek na recept koji se koristi za profilaktički tretman migrenskih glavobolja.

Metisergid
(IUPAC) ime
1-Metil- d-liserginska kiselina- (1-hydroxybut- 2-il) amid
Klinički podaci
AHFS/Drugs.com Mikromedeks, detaljne potrošačke informacije
MedlinePlus a603022
Identifikatori
CAS broj 361-37-5
ATC kod N02CA04
PubChem[1][2] 9681
DrugBank DB00247
ChemSpider[3] 9300
UNII XZA9HY6Z98 DaY
KEGG[4] D02357 DaY
ChEMBL[5] CHEMBL1065 DaY
Hemijski podaci
Formula C21H27N3O2 
Mol. masa 353,458 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Farmakologija uredi

Metisergid formira interakcije sa serotoninskim (5-HT) receptorima. Njegovo terapeutsko dejstvo u migrenskoj profilaksi je vezano za njegov antagonizam na 5-HT2B receptoru.[6] Osim toga, on je antagonist na 5-HT2C i 5-HT1A receptoru.[7][8] Poznato je da je parcijalni agonist na još nekim 5-HT receptorima.[9] Metisergid se metabolizuje u metilergometrin u ljudskom telu, koji je odgovoran za njegove psihodelične efekte.[10]

Vidi još uredi

Reference uredi

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. Schmuck K, Ullmer C, Kalkman HO, Probst A, Lubbert H (May 1996). „Activation of meningeal 5-HT2B receptors: an early step in the generation of migraine headache?”. Eur. J. Neurosci. 8 (5): 959–67. DOI:10.1111/j.1460-9568.1996.tb01583.x. PMID 8743744. 
  7. Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 187
  8. Saxena PR, Lawang A (October 1985). „A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors”. Arch Int Pharmacodyn Ther 277 (2): 235–52. PMID 2933009. 
  9. Colpaert FC, Niemegeers CJ, Janssen PA (October 1979). „In vivo evidence of partial agonist activity exerted by purported 5-hydroxytryptamine antagonists”. Eur. J. Pharmacol. 58 (4): 505–9. DOI:10.1016/0014-2999(79)90326-1. PMID 510385. 
  10. Bredberg, U.; Eyjolfsdottir, G. S., Paalzow, L., Tfelt-Hansen, P., Tfelt-Hansen, V. (1986-01-01). „Pharmacokinetics of methysergide and its metabolite methylergometrine in man”. European Journal of Clinical Pharmacology 30 (1): 75–77. DOI:10.1007/BF00614199. PMID 3709634. 

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