Pramipeksol

Pramipeksol
(IUPAC) ime
	(S)-N6-propyl-4,5,6,7-tetrahidro-1,3-benzotiazol-2,6-diamin
Klinički podaci
Robne marke	Mirapex
AHFS/Drugs.com	Monografija
MedlinePlus	a697029
Identifikatori
CAS broj	104632-26-0
ATC kod	N04BC05
PubChem	119570
DrugBank	APRD00156
ChemSpider	106770
UNII	83619PEU5T
KEGG	D05575
ChEBI	CHEBI:8356
ChEMBL	CHEMBL301265
Hemijski podaci
Formula	C10H17N3S
Mol. masa	211,324 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C10H17N3S/c1-2-5-12-7-3-4-8-9(6-7)14-10(11)13-8/h7,12H,2-6H2,1H3,(H2,11,13)/t7-/m0/s1 ; Key: FASDKYOPVNHBLU-ZETCQYMHSA-N
Farmakokinetički podaci
Bioraspoloživost	>90%
Vezivanje za proteine plazme	15%
Poluvreme eliminacije	8-12 sata
Izlučivanje	Urin (90%), Fekalije (2%)
Farmakoinformacioni podaci
Trudnoća	B3(AU) C(US)
Pravni status	℞ Prescription only
Način primene	Oralno

Pramipeksol (Mirapeks, Mirapeksin, Sifrol) je dopaminski agonist koji se koristi za lečenje rane faze Parkinsonove bolesti i sindroma nemirnih nogu.^[6] Poznato je da se on koristi i za lečenje jake glavobolje i za neutralisanje psihičkih problema izazvanih impotencijom, koju doživljavaju neki od korisnika antidepresanata ili selektivnih inhibitora preuzimanja serotonina, mada pramipeksol zvanično nije odobren za lečenje tih poremećaja.^[7]

Pramipeksol je u jednoj pilot placebo kontrolisanoj studiji sprovedenoj radi potvrde koncepta u manično-depresivnoj psihozi pokazao da ima snažno dejstvo.^[8] On se takođe ispituje za primenu u lečenju kliničke derpesije i fibromialgije.^[9]^[10]^[11]

Hemija

Pramipreksol se može sintetisati iz cikloheksanonskih derivata na sledeći način:^[12]

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
↑ National Prescribing Service (2009). "Pramipexole for Parkinson's Disease". Medicines Update. Available at http://www.nps.org.au/consumers/publications/medicine_update/issues/Pramipexole_for_Parkinsons_disease
↑ DeBattista C, Solvason HB, Breen JA, Schatzberg AF. (2000). „Pramipexole augmentation of a selective serotonin reuptake inhibitor in the treatment of depression.”. J Clin Psychopharmacol. 20 (2): 274–275. DOI:10.1097/00004714-200004000-00029. PMID 10770475.
↑ Zarate CA, Payne JL, Singh J, et al. (July 2004). „Pramipexole for bipolar II depression: a placebo-controlled proof of concept study”. Biol. Psychiatry 56 (1): 54–60. DOI:10.1016/j.biopsych.2004.03.013. PMID 15219473.
↑ Lattanzi L, Dell'Osso L, Cassano P, Pini S, Rucci P, Houck PR, Gemignani A, Battistini G, Bassi A, Abelli M, Cassano GB. (2002). „Pramipexole in treatment-resistant depression: a 16-week naturalistic study.”. Bipolar Disord. 4 (5): 307–314. DOI:10.1034/j.1399-5618.2002.01171.x. PMID 12479663.
↑ Cassano P, Lattanzi L, Soldani F, Navari S, Battistini G, Gemignani A, Cassano GB. (2004). „Pramipexole in treatment-resistant depression: an extended follow-up.”. Depression and Anxiety 20 (3): 131–138. DOI:10.1002/da.20038. PMID 15549689.
↑ Holman AJ, Myers RR. (2005). „A randomized, double-blind, placebo-controlled trial of pramipexole, a dopamine agonist, in patients with fibromyalgia receiving concomitant medications.”. Arthritis Rheum. 52 (8): 2495–2505. DOI:10.1002/art.21191. PMID 16052595.
↑ Schneider Claus, Mierau Joachim (1987). „Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analog of apomorphine”. Journal of Medicinal Chemistry 30 (3): 494–8. DOI:10.1021/jm00386a009. PMID 3820220.

Povezano

Dekspramipeksol, enantiomer pramiproksola
Piribedil
Ropinirol
Rotigotin

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Mirapeks Arhivirano 2009-06-28 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

[6] National Prescribing Service (2009). "Pramipexole for Parkinson's Disease". Medicines Update. Available at http://www.nps.org.au/consumers/publications/medicine_update/issues/Pramipexole_for_Parkinsons_disease

[pmid10770475-7] DeBattista C, Solvason HB, Breen JA, Schatzberg AF. (2000). „Pramipexole augmentation of a selective serotonin reuptake inhibitor in the treatment of depression.”. J Clin Psychopharmacol. 20 (2): 274–275. DOI:10.1097/00004714-200004000-00029. PMID 10770475.

[8] Zarate CA, Payne JL, Singh J, et al. (July 2004). „Pramipexole for bipolar II depression: a placebo-controlled proof of concept study”. Biol. Psychiatry 56 (1): 54–60. DOI:10.1016/j.biopsych.2004.03.013. PMID 15219473.

[pmid12479663-9] Lattanzi L, Dell'Osso L, Cassano P, Pini S, Rucci P, Houck PR, Gemignani A, Battistini G, Bassi A, Abelli M, Cassano GB. (2002). „Pramipexole in treatment-resistant depression: a 16-week naturalistic study.”. Bipolar Disord. 4 (5): 307–314. DOI:10.1034/j.1399-5618.2002.01171.x. PMID 12479663.

[pmid15549689-10] Cassano P, Lattanzi L, Soldani F, Navari S, Battistini G, Gemignani A, Cassano GB. (2004). „Pramipexole in treatment-resistant depression: an extended follow-up.”. Depression and Anxiety 20 (3): 131–138. DOI:10.1002/da.20038. PMID 15549689.

[pmid16052595-11] Holman AJ, Myers RR. (2005). „A randomized, double-blind, placebo-controlled trial of pramipexole, a dopamine agonist, in patients with fibromyalgia receiving concomitant medications.”. Arthritis Rheum. 52 (8): 2495–2505. DOI:10.1002/art.21191. PMID 16052595.

[12] Schneider Claus, Mierau Joachim (1987). „Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analog of apomorphine”. Journal of Medicinal Chemistry 30 (3): 494–8. DOI:10.1021/jm00386a009. PMID 3820220.

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