Metisergid

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	9681
DrugBank	DB00247
ChemSpider	9300
UNII	XZA9HY6Z98
KEGG	D02357
ChEMBL	CHEMBL1065
Hemijski podaci
Formula	C21H27N3O2
Mol. masa	353,458 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C21H27N3O2/c1-4-15(12-25)22-21(26)14-8-17-16-6-5-7-18-20(16)13(10-23(18)2)9-19(17)24(3)11-14/h5-8,10,14-15,19,25H,4,9,11-12H2,1-3H3,(H,22,26)/t14-,15+,19-/m1/s1 ; Key: KPJZHOPZRAFDTN-ZRGWGRIASA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

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

Farmakologija

Metisergid formira interakcije sa serotoninskim (5-HT) receptorima. Njegovo terapeutsko dejstvo u migrenskoj profilaksi je vezano za njegov antagonizam na 5-HT_2B receptoru.^[6] Osim toga, on je antagonist na 5-HT_2C i 5-HT_1A 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]

Povezano

Triptan

Reference

↑ 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
↑ 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.
↑ 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
↑ 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.
↑ 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
↑ 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.
↑ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 187
↑ 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.
↑ 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.
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Novartis Sansert site Arhivirano 2005-12-13 na Wayback Machine-u.
Novartis Sansert product description Arhivirano 2006-12-16 na Wayback Machine-u.

[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

[pmid8743744-6] 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.

[Rang187-7] Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 187

[pmid2933009-8] 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.

[pmid510385-9] 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.

[1]