WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 315247
Description: Pergolide (Permax, Pergotoliderived) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with low levels of the neurotransmitter dopamine in the brain. Pergolide has some of the same effects as dopamine in the body. In 2007, pergolide was withdrawn from the U.S. market after several published studies revealed a link between the drug and increased rates of valvular dysfunction. (Source: http://en.wikipedia.org/wiki/Pergolide )
MedKoo Cat#: 315247
Chemical Formula: C19H26N2S
Exact Mass: 314.18167
Elemental Analysis: C, 72.56; H, 8.33; N, 8.91; S, 10.20
Related CAS #: 423748-02-1 (mesylate salt) 66104-22-1 (free base)
IUPAC/Chemical Name: 9-((methylthio)methyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline
InChi Key: YEHCICAEULNIGD-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: CCCN1CC(CSC)CC2C3=CC=CC4=C3C(CC12)=CN4
Permax (Pergolide Mesylate) is an ergot derivative dopamine receptor agonist at both D1 and D2 receptor sites. Pergolide mesylate is chemically designated as 8B-[(Methylthio)methyl]-6-propylergoline monomethanesulfonate. The formula weight of the base is 314.5; 1 mg of base corresponds to 3.18 Âµmol. Permax is provided for oral administration in tablets containing 0.05 mg (0.159 Âµmol), 0.25 mg (0.795 Âµmol), or 1 mg (3.18 Âµmol) pergolide as the base. The tablets also contain croscarmel lose sodium, iron oxide, lactose, magnesium stearate, and povidone. The 0.05-mg tablet also contains methionine, and the 0.25mg tablet also contains FD&C Blue No.2.
Pharmacodynamic Information: Pergolide mesylate is a potent dopamine receptor agonist. Pergolide is 10 to 1,000 times more potent than bromocriptine on a milligram per milligram basis in various in vitro and in vivo test systems. Pergolide mesylate inhibits the secretion of prolactin in humans; it causes a transient rise in serum concentrations of growth hormone and a decrease in serum concentrations of luteinizing hormone. In ParkinsonÂ†s disease, pergolide mesylate is believed to exert its therapeutic effect by directly stimulating postsynaptic dopamine receptors in the nigrostriatal system. Pharmacokinetic Information (Absorption, Distribution, Metabolism, and Elimination): Information on oral systemic bioavailability of pergolide mesylate is unavailable because of the lack of a sufficiently sensitive assay to detect the drug after the administration of a single dose. However, following oral administration of 14C radiolabeled pergolide mesylate, approximately 55% of the administered radioactivity can be recovered from the urine and 5% from expired CO2, suggesting that a significant fraction is absorbed. Nothing can be concluded about the extent of presystemic clearance, if any. At least 10 metabolites have been detected, including N-despropyl-pergolide, pergolide sulfoxide, and pergolide sulfone. Perolide sulfoxide and pergolide sulfone are dopamine agonists in animals. The other detected metabolites have not been identified and it is not known whether any other metabolites are active pharmacologically. The major route of excretion is the kidney. Pergolide is approximately 90% bound to plasma proteins. This extent of protein binding may be important to consider when pergolide mesylate is coadministered with other drugs known to affect protein binding.