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91374-20-8

91374-20-8 structure
91374-20-8 structure
  • Name: Ropinirole hydrochloride
  • Chemical Name: 4-(2-(Dipropylamino)ethyl)indolin-2-one hydrochloride
  • CAS Number: 91374-20-8
  • Molecular Formula: C16H25ClN2O
  • Molecular Weight: 296.836
  • Catalog: Biochemical Inhibitor Neuronal Signaling Dopamine Receptor Agonist
  • Create Date: 2019-01-19 19:56:31
  • Modify Date: 2024-01-02 11:41:09
  • 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 from the side of injection) asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in marmosets [1]. Ropinirole (2 mg/kg, i.p.) for 7 days increases GSH, catalase and SOD activities in the striatum and protected striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in mice [2]. Ropinirole (0.2 mg/kg, i.p.) improves the use of previously akinetic forelimb and produced robust circling behavior in lesioned rats with striatal over-expression of both D2R and D3R compared to lesioned animals that received blank vector. The subtherapeutic dose of ropinirole generates only modest motor effects in lesioned rats with sole over-expression of D2R or D3R [3]. Ropinirole (1-8 mg t.i.d.) is rapidly and completely absorbed with oral bioavailability of 55%, clearance of 780 mL/min, elimination half-life of 6 hours in healthy volunteer. Since the major route of elimination for Ropinirole is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, inhibition of the former and possibly the latter may reduce the agent's clearance and lead to drug accumulation [4].
Name 4-(2-(Dipropylamino)ethyl)indolin-2-one hydrochloride
Synonyms 2H-Indol-2-one, 4-[2-(dipropylamino)ethyl]-1,3-dihydro-, hydrochloride (1:1)
4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one hydrochloride
4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one hydrochloride (1:1)
4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-onhydrochlorid
UNII-D7ZD41RZI9
ropinirole hcl
4-[2-(dipropylamino)éthyl]-1,3-dihydro-2H-indol-2-one chlorhydrate
Adartrel
MFCD01754173
Ropinirole hydrochloride
2H-indol-2-one, 4-[2-(dipropylamino)ethyl]-1,3-dihydro-, monohydrochloride
Requip
Ropinirole (hydrochloride)
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 from the side of injection) asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in marmosets [1]. Ropinirole (2 mg/kg, i.p.) for 7 days increases GSH, catalase and SOD activities in the striatum and protected striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in mice [2]. Ropinirole (0.2 mg/kg, i.p.) improves the use of previously akinetic forelimb and produced robust circling behavior in lesioned rats with striatal over-expression of both D2R and D3R compared to lesioned animals that received blank vector. The subtherapeutic dose of ropinirole generates only modest motor effects in lesioned rats with sole over-expression of D2R or D3R [3]. Ropinirole (1-8 mg t.i.d.) is rapidly and completely absorbed with oral bioavailability of 55%, clearance of 780 mL/min, elimination half-life of 6 hours in healthy volunteer. Since the major route of elimination for Ropinirole is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, inhibition of the former and possibly the latter may reduce the agent's clearance and lead to drug accumulation [4].
Related Catalog
References

[1]. Eden, R.J., et al., Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav, 1991. 38(1): p. 147-54.

[2]. Iida, M., et al., Dopamine D2 receptor-mediated antioxidant and neuroprotective effects of ropinirole, a dopamine agonist. Brain Res, 1999. 838(1-2): p. 51-9.

[3]. Lam, Y.W., Clinical pharmacology of dopamine agonists. Pharmacotherapy, 2000. 20(1 Pt 2): p. 17S-25S.

[4]. Allen, R., et al., Ropinirole decreases periodic leg movements and improves sleep parameters in patients with restless legs syndrome. Sleep, 2004. 27(5): p. 907-14.
Boiling Point 410.5ºC at 760mmHg
Melting Point 241-243ºC
Molecular Formula C16H25ClN2O
Molecular Weight 296.836
Exact Mass 296.165527
PSA 32.34000
LogP 3.78570
Storage condition Room temp

CHEMICAL IDENTIFICATION

RTECS NUMBER :
NM3288250
CHEMICAL NAME :
2H-Indol-2-one, 1,3-dihydro-4-(2-(dipropylamino)ethyl)-, monohydrochloride
CAS REGISTRY NUMBER :
91374-20-8
LAST UPDATED :
199807
DATA ITEMS CITED :
9

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
396 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1725,199
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
71 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1725,199 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1500 mg/kg/30D-I
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in adrenal weight Related to Chronic Data - changes in ovarian weight
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1731,199
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
18250 mg/kg/1Y-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Kidney, Ureter, Bladder - other changes Endocrine - changes in adrenal weight
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1731,199
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
450 mg/kg/30D-I
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - excitement Skin and Appendages - hair
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1741,199
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
5475 mg/kg/1Y-I
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - changes in ovarian weight Related to Chronic Data - changes in testicular weight
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1741,199 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
3040 mg/kg
SEX/DURATION :
female 2 week(s) pre-mating - 20 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1747,199
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1 gm/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1747,199
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
280 mg/kg
SEX/DURATION :
female 15-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1747,199
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H400
Precautionary Statements P301 + P312 + P330
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn,N
Risk Phrases R22
Safety Phrases 36-60-61-37/39-26
RIDADR UN 3077 9/PG 3
RTECS NM3288250
Hazard Class 9.0
HS Code 2933790090
91374-25-3 structure

91374-25-3

~89%

91374-20-8 structure

91374-20-8
Literature: IND-SWIFT LABORATORIES LIMITED Patent: WO2008/84499 A1, 2008 ; Location in patent: Page/Page column 8 ;
142-84-7 structure

142-84-7
120427-96-5 structure

120427-96-5

~50%

91374-20-8 structure

91374-20-8
Literature: TORRENT PHARMACEUTICALS LTD Patent: WO2005/80333 A1, 2005 ; Location in patent: Page/Page column 23 ;
142-84-7 structure

142-84-7
120427-95-4 structure

120427-95-4

~%

91374-20-8 structure

91374-20-8
Literature: WO2011/30330 A2, ; Page/Page column 9 ;
91374-21-9 structure

91374-21-9

~%

91374-20-8 structure

91374-20-8
Literature: WO2005/40115 A1, ; Page/Page column 6 ;
863436-07-1 structure

863436-07-1

~40%

91374-20-8 structure

91374-20-8
Literature: Helm AG; CF Pharma Gyogyszergyarto Kft. Patent: EP1568689 A1, 2005 ; Location in patent: Page/Page column 7 ;
142-84-7 structure

142-84-7
139122-20-6 structure

139122-20-6

~85%

91374-20-8 structure

91374-20-8
Literature: Hayler, John D.; Howie, Simon L. B.; Giles, Robert G.; Negus, Alan; Oxley, Paul W.; Walsgrove, Timothy C.; Whiter Organic Process Research and Development, 1998 , vol. 2, # 1 p. 3 - 9
920986-68-1 structure

920986-68-1

~%

91374-20-8 structure

91374-20-8
Literature: WO2011/72704 A1, ;
139122-17-1 structure

139122-17-1

~%

91374-20-8 structure

91374-20-8
Literature: Organic Process Research and Development, , vol. 2, # 1 p. 3 - 9
139122-18-2 structure

139122-18-2

~%

91374-20-8 structure

91374-20-8
Literature: Organic Process Research and Development, , vol. 2, # 1 p. 3 - 9
HS Code 2933790090
Summary 2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

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