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Ropinirole hydrochloride

Ropinirole hydrochloride structure

CAS No:
91374-20-8
Formula:
C16H24N2O.ClH
Chemical Name:
Ropinirole hydrochloride
Synonyms:
2H-Indol-2-one,4-[2-(dipropylamino)ethyl]-1,3-dihydro-,hydrochloride (1:1);2H-Indol-2-one,4-[2-(dipropylamino)ethyl]-1,3-dihydro-,monohydrochloride;SKF 101468 hydrochloride;Ropinirole hydrochloride;SKF 101468A;Requip;Parkirop;Ropitar;Ropark;Repreve;Ronirol;Adartrel;Spiroco XL;Ralnea XL;Clevor;115616-44-9
Categories:
Biochemical Engineering > Inhibitors

Description

Ropinirole hydrochloride(SKF101468 hydrochloride) a selective dopamine D2 receptor inhibitor with IC50 of 29 nM.Target: Dopamine D2 ReceptorRopinirole (50 mg/kg, i.p.) causes biphasic spontaneous locomotor activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently inhibits the dyskinesias induced by 2-di-n-propylamino-5,6-di-hydroxytetralin in mice. Ropirtirole, at doses of 1 and 10 μg, injected unilaterally directly into the striatum of the rat causes marked, contralateral (away

Ropinirole hydrochloride is a member of indoles.|Ropinirole is a selective dopamine receptor agonist used in the therapy of Parkinson disease. Ropinirole therapy is associated with low rate of transient serum enzyme elevations during treatment and has been implicated in rare cases of acute liver injury.|Ropinirole Hydrochloride is the hydrochloride salt form of ropinirole, a non-ergot dopamine agonist with antiparkinsonian property. Acting as a substitute for dopamine, ropinirole hydrochloride binds to and activates dopamine D2 and D3 receptors within the caudate putamen in the brain, thereby improving motor function.

Ropinirole hydrochloride Basic Attributes

Molecular Weight：

296.84

Exact Mass：

296.165527

EC Number：

1308068-626-2

UNII：

D7ZD41RZI9

DSSTox ID：

DTXSID50238533

NCI Thesaurus Code：

C47710

ATC Code：

QN04BC04

HScode：

2933790090

Characteristics

PSA：

32.3

XLogP3：

3.78570

Appearance：

light yellow

Melting Point：

241-243 °C

Boiling Point：

410.5°C at 760 mmHg

Water Solubility：

H2O: >10mg/mL

Storage Conditions：

room temp

Safety Information

Packing level：

Ⅲ

Transport codes：

UN30779/PG3

wgk germany：

hazard class code：

22-50/53-36/38

safety instructions：

36-60-61-37/39-26

RTECS Number：

NM3288250

Marks：

Xn,N,Xi

Precautionary statement(s)：

P301 + P312 + P330

Hazard Statements：

H302-H400

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, P391, and P501|Aggregated GHS information provided by 47 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Hepatotoxicity：

Ropinirole has been reported to cause serum aminotransferase or alkaline phosphatase elevations in a small proportion of patients, but these abnormalities are usually mild, asymptomatic and self-limiting even without dose adjustment. Ropinirole has been implicated in a small number of cases of acute liver injury, but the clinical characteristics and typical pattern of enzyme elevations has not been characterized. In one case report, the time to onset was 2 months and the pattern of liver enzyme elevations was mixed and associated with marked jaundice. Immunoallergic and autoimmune features were not present. The injury resolved within 2 months of stopping. Thus, ropinirole can cause acute, clinically apparent liver injury with jaundice, but it is rare.

Drug Information

Drug Indication：

Induction of vomiting in dogs.,

LiverTox Summary：

Ropinirole is a selective dopamine receptor agonist used in the therapy of Parkinson disease. Ropinirole 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：

Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists. (See all compounds classified as Antiparkinson Agents.)|Drugs that bind to and activate dopamine receptors. (See all compounds classified as Dopamine Agonists.)

MeSH Entry Terms：

4-(2-(di-n-propylamino)ethyl)-2(3H)-indolone

Ropinirole hydrochloride Use and Manufacturing

Uses

antiparkinsonian;non-ergoline D2, D3, and D4 dopamine receptor agonist with highest affinity for D3

Use Classification：

Veterinary drugs -> Clevor -> EMA Drug Category|Dopaminergic agents, Dopamine agonists -> Veterinary pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:296.83
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:7
Exact Mass:296.1655411
Monoisotopic Mass:296.1655411
Topological Polar Surface Area:32.3
Heavy Atom Count:20
Complexity:287
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Activates dopamine receptors in the central nervous system; acute toxicity LD50 in rats and mice is 867 and 662 mg/kg respectively; long-term toxicity studies have shown that high doses (15 mg/kg/day) may cause weight loss and pathological changes in the testicles and ovaries, which may be related to the inhibition of prolactin. The main toxic reactions are related to dopamine receptor stimuli.

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

Ropinirole hydrochloride extended-release tablets
Ingredients	Ropinirole hydrochloride. Chemical name: 4-[2-(di-n-propylamino)-ethyl]-1,3-dihydro-2H-indol-2-one hydrochloride Molecular weight: C16H24N2OHCl
Indication	P450 action: In vitro studies have found that CYP1A2 is the enzyme that plays a major role in the metabolism of ropinirole. Taking CYP1A2 substrates or inhibitors will change the clearance rate of ropinirole. Therefore, the dose of ropinirole should be adjusted accordingly when stopping or using strong CYP1A2 inhibitors.
Specifications	2mg

Ropinirole hydrochloride
Manufacturer	Zein BIOTECHNOLOGY Co., Ltd.

Ropinirole hydrochloride extended-release tablets
Specifications	8mg

See More Related Drugs

Registered Holders

SYNTHIMED LABS PRIVATE LTD

United States
Active
ALIVUS LIFE SCIENCES LTD

United States
Active
ALEMBIC PHARMACEUTICALS LTD

United States
Active

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