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Pergolide mesylate

Pergolide mesylate structure

CAS No:
66104-23-2
Formula:
C19H26N2S.CH4O3S
Chemical Name:
Pergolide mesylate
Synonyms:
Ergoline,8-[(methylthio)methyl]-6-propyl-,(8β)-,monomethanesulfonate;Indolo[4,3-fg]quinoline,ergoline deriv.;Pergolide mesylate;LY 127809;Pergolide methanesulfonate;Permax;Celance;NSC 319773;138932-34-0
Categories:
Biochemical Engineering > Inhibitors

Description

Pergolide Mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist.Target: Dopamine ReceptorPergolide mesylate (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Pergolide mesylate functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabe

Pergolide mesylate is a methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction. It has a role as an antiparkinson drug, a dopamine agonist and a geroprotector. It contains a pergolide(1+).|Pergolide is an oral dopamine receptor agonist used predominantly in the therapy of Parkinson disease. Pergolide therapy is associated with low rate of transient serum enzyme elevations during treatment and has been implicated in rare cases of acute liver injury.|Pergolide Mesylate is a semi-synthetic ergot derivative and a dopamine agonist with antiparkinson property. Pergolide mesylate binds to and activates dopamine receptor subtypes D1 and D2, resulting in prolactin secretion inhibition, transient increase in serum concentration of growth hormone, and decrease in serum concentration of luteinizing hormone. Direct stimulation of postsynaptic dopamine receptors in the nigrostriatal system, may account for this agent's antiparkinson activity.|A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.

Pergolide mesylate Basic Attributes

Molecular Weight：

410.59

Exact Mass：

410.169769

UNII：

55B9HQY616

NSC Number：

758442|319773

DSSTox ID：

DTXSID6040583

NCI Thesaurus Code：

C47665

HScode：

2939690000

Characteristics

PSA：

107

XLogP3：

4.79380

Appearance：

white

Melting Point：

225 °C

Boiling Point：

491.3ºC at 760 mmHg

Flash Point：

250.9ºC

Water Solubility：

ethanol: soluble 2mg/mL

Storage Conditions：

−20°C

Specific rotation：

aD20 between -18.0° and -23.0° (c = 10 mg/ml in DMF)

Collision Cross Section：

177.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

UN 1544

wgk germany：

hazard class code：

safety instructions：

28-36/37-45

RTECS Number：

KE6345000

Marks：

T+

Precautionary statement(s)：

Missing Phrase - N15.00950417

Hazard Statements：

H300

GHS Classification：

|Danger|H300 (97.62%): Fatal if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 42 companies from 4 notifications to the ECHA C&L Inventory.|H300: Fatal if swallowed [Danger Acute toxicity, oral]

Toxicity

Hepatotoxicity：

Pergolide has been reported to cause serum aminotransferase elevations in a small proportion of patients, but these abnormalities are usually mild, asymptomatic and self-limiting even without dose adjustment. In addition, pergolide has been implicated in a small number of cases of clinically apparent, acute liver injury, but the frequency, severity, clinical characteristics and typical pattern of enzyme elevations have not been characterized. Thus, pergolide is may be a rare cause of clinically apparent liver injury.

Drug Information

LiverTox Summary：

Pergolide is an oral dopamine receptor agonist used predominantly in the therapy of Parkinson disease. Pergolide therapy is associated with low rate of transient serum enzyme elevations during treatment and has been implicated in rare cases of acute liver injury.

Drug Classes：

Antiparkinson Agents

MeSH：

Drugs that bind to and activate dopamine receptors. (See all compounds classified as Dopamine Agonists.)

MeSH Entry Terms：

Celance

Pergolide mesylate Use and Manufacturing

Uses

dopamine receptor agonist, anti-Parkinson's agent

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Animal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients

Computed Properties

Molecular Weight:410.6
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:4
Exact Mass:410.16978517
Monoisotopic Mass:410.16978517
Topological Polar Surface Area:107
Heavy Atom Count:27
Complexity:480
Defined Atom Stereocenter Count:3
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Pergolide is a typical central nervous system postsynaptic dopamine receptor agonist that can significantly inhibit the release of prolactin from the anterior pituitary and reduce the serum prolactin content of normal and reserpine-treated rats; it reduces the metabolic conversion of dopamine in the rat brain, thereby reducing the content of 3,4-dihydroxyphenylacetic acid in the brain, causing rats with nigrostriatal damage to produce a contralateral rotation response; it increases the autonomous activity and climbing behavior of mice, causes stereotypic animals in rats and guinea pigs, and counteracts spontaneous tremors caused by ventral damage to the midbrain dorsal tegmentum of monkeys.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Pergolide Mesylate Tablets
Ingredients	The main ingredient of this product is pergolide mesylate. Molecular weight: C19H26N2S·CH3SO3H
Indication	If used with other drugs, drug interactions may occur. Please consult your doctor or pharmacist for details.
Specifications	0.25mg*30s

Registered Holders

TAPI Czech Industries s.r.o.

Czech
Active
OLON S.P.A.

Italy
Active
Chemwerth Inc.

European Union
Active

See More Registered Holders

Recommended Suppliers of Pergolide mesylate

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CN
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CAS No.: 66104-23-2

Grade: Industrial Grade

Content: 99%

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