Kabergolin

Kabergolin
(IUPAC) ime
	N-[3-(Dimetilamino)propil]-N-[(etilamino)karbonil]- 6-(2-propenil)-8g-ergolin-8-karboksamid; ili; 1-[(6-alilergolin8β-il)- karbonil]-1- [3-(dimetilamino)propil]-3-etilurea
Klinički podaci
AHFS/Drugs.com	Monografija
Identifikatori
CAS broj	81409-90-7
ATC kod	G02CB03 N04BC06
PubChem	54746
DrugBank	APRD00836
ChemSpider	49452
UNII	LL60K9J05T
KEGG	D00987
ChEBI	CHEBI:3286
ChEMBL	CHEMBL1201087
Hemijski podaci
Formula	C26H37N5O2
Mol. masa	451,604 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21-,23-/m1/s1 ; Key: KORNTPPJEAJQIU-KJXAQDMKSA-N
Farmakokinetički podaci
Bioraspoloživost	Primetan je efekat prvog prolaza; apsolutna biodostupnost nije poznata
Vezivanje za proteine plazme	Umereno vezivanje (40% do 42%); nezavisno od koncentracije
Metabolizam	Hepatički, predominatno putem hidrolize veze acilureje ili ureje
Poluvreme eliminacije	63-69 časa (procena)
Izlučivanje	Urin (22%), fekalije (60%)
Farmakoinformacioni podaci
Licenca	US FDA:link
Trudnoća	B(US)
Pravni status	℞-only (SAD)
Način primene	Oralno

Kabergolin (Dostineks, Kabaser) je ergotni derivat, koji je potentan agonist dopaminskog receptora D2. In vitro ispitivanja su pokazala da kabergolin ima direktno inhibitorno dejstvo na hipofizne prolaktinske ćelije.^[6] On se često koristi kao početni agens u tretmanu prolaktinoma usled njegove visokog afiniteta za D2 mesta receptora, manje izraženih nuspojava, i podesnijeg režima doziranja u odnosu na stariji bromokriptin.

Farmakologija

Mada je kabergolin široko poznat uglavnom kao dopaminski agonist D₂ receptora, on takođe poseduje znatan afinitet za D₃, D₄, 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, α_2B- receptore, i umeren/nizak afinitet za D₁ i 5-HT₇ receptore. Kabergolin deluje kao agonist svih receptora izuzev 5-HT₇ i α_2B-, na kojima je antagonist.^[7]

Izvori

↑ 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
↑ „Dostinex at www.rxlist.com”. Arhivirano iz originala na datum 2007-05-06. Pristupljeno 27. 4. 2007.
↑ Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C (March 2009). „Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes”. Experimental Eye Research 88 (3): 386–97. DOI:10.1016/j.exer.2008.10.003. PMID 18992242.

Povezano

Bromokriptin

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Kabergolin

[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

[Dostinex_at_www.rxlist.com-6] „Dostinex at www.rxlist.com”. Arhivirano iz originala na datum 2007-05-06. Pristupljeno 27. 4. 2007.

[pmid18992242-7] Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C (March 2009). „Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes”. Experimental Eye Research 88 (3): 386–97. DOI:10.1016/j.exer.2008.10.003. PMID 18992242.

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