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Mirapex

Pramipexole
Pramipexole.svg
Pramipexole ball-and-stick model.png
Clinical data
Trade names Mirapex, Mirapexin, Sifrol
AHFS/Drugs.com Monograph
MedlinePlus a697029
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code N04BC05 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability >90%
Protein binding 15%
Biological half-life 8–12 hours
Excretion Urine (90%), Feces (2%)
Identifiers
CAS Number 104632-26-0 YesY
PubChem (CID) 119570
IUPHAR/BPS 953
DrugBank DB00413 YesY
ChemSpider 106770 YesY
UNII 83619PEU5T YesY
KEGG D05575 YesY
ChEBI CHEBI:8356 YesY
ChEMBL CHEMBL301265 YesY
ECHA InfoCard 100.124.761
Chemical and physical data
Formula C10H17N3S
Molar mass 211.324 g/mol
3D model (Jmol) Interactive image
  

Pramipexole (Mirapex, Mirapexin, Sifrol) is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS).

Pramipexole acts as a partial/full agonist at the following receptors:

Pramipexole also possesses low/insignificant affinity (500–10,000 nM) for the 5-HT1A, 5-HT1B, 5-HT1D, and α2-adrenergic receptors. It has negligible affinity (>10,000 nM) for the D1, D5, 5-HT2, α1-adrenergic, β-adrenergic, H1, and mACh receptors. All sites assayed were done using human tissues.

While pramipexole is used clinically (see below), its D3-preferring receptor binding profile has made it a popular tool compound for preclinical research. For example, pramipexole has been used (in combination with D2- and or D3-preferring antagonists) to discover the role of D3 receptor function in rodent models and tasks for neuropsychiatric disorders. Of note, it appears that pramipexole, in addition to having effects on dopamine D3 receptors, may also affect mitochondrial function via a mechanism that remains less understood. A pharmacological approach to separate dopaminergic from non-dopaminergic (e.g. mitochondrial) effects of pramipexole has been to study the effects of the R-stereoisomer of pramipexole (which has much lower affinity to the dopamine receptors when compared to the S-isomer) side-by-side with the effects of the S-isomer.


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Wikipedia

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