Pergolide Mesylate

Pergolide Mesylate

Cat Number
API0232220
CAS Number
66104-23-2

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CAS Number
66104-23-2
EINECS
636-270-7
Storage
Store at 2-8°C
Synonyms
Pergolide Methanesulfonate; Pergolide mesilate; DTXSID6040583; LY127809; NSC-319773; NSC-758442; LY-127809
Molecular Formula
C20H30N2O3S2
Molecular Weight
410.6
Smiles
CCCN1C[C@@H](C[C@H]2[C@H]1CC3=CNC4=CC=CC2=C34)CSC.CS(=O)(=O)O
Appearance
White to off-white solid
Melting Point
252-254°C
Boiling Point
491.3°C at 760 mmHg
Relative Density
1.1±0.1
General Description
Pergolide mesylate is a synthetic ergoline derivative with a methylthio group, structurally related to the ergot alkaloids. Its chemical structure is (8β)-8-[(methylthio)methyl]-6-propylergoline mesylate. Pergolide is a white to off-white powder with a molecular weight of 410.6 Da (as the mesylate). It is a long-acting dopamine receptor agonist with high affinity for D1, D2, and D3 receptors.
Mechanism of Action
Pergolide acts as a potent agonist at dopamine receptors, particularly D2 and D3, in the nigrostriatal pathway, compensating for the dopaminergic deficit in Parkinson's disease. It also has weak activity at serotonin and alpha-adrenergic receptors. The drug's prolonged action allows for once-daily dosing. Pergolide also inhibits prolactin secretion by acting on D2 receptors in the pituitary.
Application
Pergolide was indicated as an adjunct to levodopa in the treatment of Parkinson's disease and for the management of hyperprolactinemia.

Does Pergolide Mesylate require refrigerated storage as an ergoline derivative?

Yes, it should be stored at 2-8°C. At room temperature, oxidation and degradation of the indole ring occur rapidly, reducing potency.

Is Pergolide Mesylate sensitive to light and oxygen during handling?

Yes, it is highly sensitive to light and oxygen. Store in light-resistant, airtight containers under inert gas (nitrogen). Handle under subdued light.

Is Pergolide Mesylate stable in tablet formulations with standard excipients?

Yes, when formulated with antioxidants and moisture-protective packaging.

How is the impurity pergolide sulfoxide (an oxidative degradation product) monitored?

This degradation product is specifically quantified using a stability-indicating HPLC method, ensuring it remains within pharmacopoeial limits.
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