Pergolid

Pergolid
(IUPAC) ime
	(8β)-8-[(metiltio)metil]-6-propilergolin
Klinički podaci
AHFS/Drugs.com	Monografija
Identifikatori
CAS broj	66104-22-1
ATC kod	N04BC02
PubChem	47811
DrugBank	APRD00663
ChemSpider	43503
UNII	24MJ822NZ9
KEGG	D08339
ChEMBL	CHEMBL531
Hemijski podaci
Formula	C19H26N2S
Mol. masa	314,489 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H26N2S/c1-3-7-21-11-13(12-22-2)8-16-15-5-4-6-17-19(15)14(10-20-17)9-18(16)21/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3/t13-,16-,18-/m1/s1 ; Key: YEHCICAEULNIGD-MZMPZRCHSA-N
Sinonimi	(6aR,9R,10aR)-9-(metiltiometil)-7-propil-4,6,6a,7,8,9,10,10a-oktahidroindolo[4,3-fg]hinolin
Farmakokinetički podaci
Vezivanje za proteine plazme	90%
Metabolizam	Hepatički
Poluvreme eliminacije	27 sata
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Povučen sa tržišta (SAD)
Način primene	Oralno

Pergolid (Permaks) je agonist dopaminskog receptora koji je baziran na ergolinu. On se koristi u nekim zemljama za lečenje Parkinsonove bolesti.^[6]^[7] Parkinsonova bolest je vezana za niske nivoe neurotransmitera dopamina u mozgu. Pergolid u izvesnoj meri deluje poput dopamina u telu.

Pergolid je 2007. povučen sa tržišta u SAD-u kao lek za ljudsku upotrebu. Do toga je došlo nakon objavljivanja nekoliko studija koje su ukazale na vezu između leka i povišenih nivoa valvularne disfunkcije.^[6]^[8]

Pergolid je odobren za veterinarsku upotrebu^[9] na konjima za tretman Kušingovog sindroma.

Izvori uredi

↑ 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
↑ ^6,0 ^6,1 Guy Van Camp, Anja Flamez, Bernard Cosyns, Caroline Weytjens, Luc Muyldermans, Michel Van Zandijcke, Johan De Sutter, Patrick Santens, Pierre Decoodt, Christian Moerman, Danny Schoors (2004). „Treatment of Parkinson's disease with pergolide and relation to restrictive valvular heart disease”. The Lancet 363 (9416): 1179–1183.
↑ Earley CJ, Allen RP (1996). „Pergolide and carbidopa/levodopa treatment of the restless legs syndrome and periodic leg movements in sleep in a consecutive series of patients”. Sleep 19 (10): 801-10. PMID 9085489. ^{[mrtav link]}
↑ Pergolide Withdrawn From US Market
↑ Barbara Forney. „Pergolide For Veterinary Use”.

[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

[Guy_Van_Camp-6] 6,0 ^6,1 Guy Van Camp, Anja Flamez, Bernard Cosyns, Caroline Weytjens, Luc Muyldermans, Michel Van Zandijcke, Johan De Sutter, Patrick Santens, Pierre Decoodt, Christian Moerman, Danny Schoors (2004). „Treatment of Parkinson's disease with pergolide and relation to restrictive valvular heart disease”. The Lancet 363 (9416): 1179–1183.

[7] Earley CJ, Allen RP (1996). „Pergolide and carbidopa/levodopa treatment of the restless legs syndrome and periodic leg movements in sleep in a consecutive series of patients”. Sleep 19 (10): 801-10. PMID 9085489. ^{[mrtav link]}

[medscape-8] Pergolide Withdrawn From US Market

[9] Barbara Forney. „Pergolide For Veterinary Use”.

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