[CAS NO. 91374-20-8] Ropinirole hydrochloride
PRODUCTS SPECIFICATIONS [91374-20-8]
DESCRIPTION [91374-20-8]
Overview
| MDL | MFCD01754173 |
|---|---|
| Molecular Weight | 296.84 |
| Molecular Formula | C16H25ClN2O |
| SMILES | O=C1NC2=C(C(CCN(CCC)CCC)=CC=C2)C1.Cl |
Summary
Ropinirole (SKF 101468) hydrochloride is an orally active, potent D 3 /D 2 receptor agonist with a K i of 29 nM for D 2 receptor . Ropinirole hydrochloride has pEC 50 s of 7.4, 8.4 and 6.8 for hD 2 , hD 3 and hD 4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D 1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease [1] [2] .
IC50 & Target
|
D 2 Receptor 29 nM (Ki) |
hD 2 Receptor 7.4 (pEC 50 ) |
hD 3 Receptor 8.4 (pEC 50 ) |
hD 4.4 Receptor 6.8 (pEC 50 ) |
In Vitro
Ropinirole hydrochloride has affinity for D 3 receptors of 10-20 fold higher than the D 2 and D 4 receptors. Ropinirole hydrochloride is weakly active at alpha 2-adrenoceptors and 5-HT 2 receptors but inactive at 5-HT 1 , benzodiazepine and gamma-aminobutyric acid receptors or alpha 1 and beta-adrenoceptors [1] [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ropinirole (0.1-10 mg/kg; i.p.) decreases intracranial self-stimulation (ICSS) thresholds and induces anxiolytic- and antidepressive-like effects without affecting motor activity or spatial memory [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague–Dawley rats weighing 220-350 g [2] |
| Dosage: | 0.1, 1 or 10 mg/kg |
| Administration: | i.p. |
| Result: | Decreased ICSS thresholds and induced anxiolytic- and antidepressive-like effects without affecting motor activity or spatial memory. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00381472 | GlaxoSmithKline |
Parkinson Disease
|
June 2003 | Phase 3 |
| NCT00530790 | GlaxoSmithKline |
Restless Legs Syndrome
|
August 23, 2007 | Phase 2 |
| NCT01393457 | The University of Texas Health Science Center, Houston |
Cocaine Dependence
|
June 2011 | Phase 2 |
| NCT00256854 | GlaxoSmithKline |
Restless Legs Syndrome|Restless Legs Syndrome (RLS)
|
November 14, 2005 | Phase 3 |
| NCT00986245 | Seoul National University Hospital |
Parkinson Disease
|
September 2009 | Phase 4 |
| NCT00334048 | St. Luke´s-Roosevelt Hospital Center|GlaxoSmithKline |
Sexual Dysfunction
|
June 2006 | Phase 4 |
| NCT00140712 | GlaxoSmithKline |
Restless Legs Syndrome
|
June 10, 2005 | Phase 1 |
| NCT01007864 | Desitin Arzneimittel GmbH|FGK Clinical Research GmbH |
Idiopathic Parkinson´s Disease
|
January 2010 | Phase 3 |
| NCT03806530 | Population Health Research Institute |
End Stage Renal Disease|Restless Legs Syndrome
|
May 1, 2019 | Phase 3 |
| NCT00996944 | GlaxoSmithKline |
Restless Legs Syndrome
|
November 30, 2009 | Phase 2 |
| NCT01712568 | Lupin Ltd. |
Pharmacokinetic Study
|
September 2008 | Phase 1 |
| NCT00357097 | GlaxoSmithKline |
Restless Legs Syndrome|Moderate to Severe Idiopathic Restless Legs Syndrome (RLS)
|
June 2006 | Phase 3 |
| NCT01485172 | GlaxoSmithKline |
Parkinson Disease
|
January 31, 2012 | Phase 4 |
| NCT00830219 | Teva Pharmaceuticals USA |
Healthy
|
November 2004 | Phase 1 |
| NCT00639119 | University of Turku |
Unverricht-Lundborg Syndrome
|
August 2007 | Phase 2 |
| NCT01714856 | Lupin Ltd. |
Pharmacokinetic Study
|
September 2008 | Phase 1 |
| NCT00422994 | GlaxoSmithKline |
Restless Legs Syndrome
|
April 2006 | Phase 1 |
| NCT00285727 | Stanford University|Duke University|GlaxoSmithKline |
Depressive Disorder, Major
|
January 2006 | Not Applicable |
| NCT00197080 | GlaxoSmithKline |
Restless Legs Syndrome
|
June 2005 | Phase 3 |
| NCT00829504 | Teva Pharmaceuticals USA |
Healthy
|
October 2004 | Phase 1 |
| NCT00823836 | GlaxoSmithKline |
Parkinson Disease
|
March 2009 | Phase 3 |
| NCT01717235 | Lupin Ltd. |
Pharmacokinetic Study
|
September 2008 | Phase 1 |
| NCT00331149 | GlaxoSmithKline |
Parkinson Disease
|
June 20, 2006 | Phase 3 |
| NCT01327339 | GlaxoSmithKline |
Restless Legs Syndrome
|
April 1, 2006 | |
| NCT00260793 | Agarwal, Pinky, M.D.|Colorado Neurology|GlaxoSmithKline |
Parkinson´s Disease
|
November 2005 | Phase 3 |
| NCT00256893 | GlaxoSmithKline |
Fibromyalgia Syndrome, Primary
|
November 2004 | Phase 2 |
| NCT00650104 | GlaxoSmithKline |
Parkinson Disease
|
May 2002 | Phase 3 |
| NCT00363727 | GlaxoSmithKline |
Parkinson´s Disease|Parkinson Disease|Dyskinesias
|
December 2003 | Phase 3 |
| NCT00314821 | Cambridge Health Alliance|Emory University|GlaxoSmithKline |
Bipolar Disorder
|
September 2005 | Phase 4 |
| NCT01371682 | GlaxoSmithKline |
Parkinson Disease
|
September 18, 2009 | Phase 1 |
| NCT00674310 | Roxane Laboratories|West-Ward Pharmaceutical |
Parkinson´s Disease|Restless Leg Syndrome
|
February 2004 | Not Applicable |
| NCT01435915 | GlaxoSmithKline |
Parkinson Disease
|
June 28, 2010 | Phase 1 |
| NCT00367822 | Axxonis Pharma AG |
Restless Legs Syndrome
|
Phase 3 | |
| NCT00632736 | GlaxoSmithKline |
Parkinson Disease|Parkinson´s Disease
|
February 2004 | Phase 3 |
| NCT00225862 | GlaxoSmithKline |
Restless Legs Syndrome
|
January 2005 | Phase 3 |
| NCT00335205 | Sheba Medical Center|Jerusalem Mental Health Center |
Bipolar Disorder|Major Depressive Disorder
|
April 2003 | Phase 4 |
| NCT01929317 | GlaxoSmithKline |
Parkinson Disease
|
August 28, 2013 | Phase 3 |
| NCT00329602 | GlaxoSmithKline |
Restless Legs Syndrome
|
March 2006 | Phase 4 |
| NCT00036218 | Pfizer |
Parkinson Disease
|
December 2001 | Phase 3 |
| NCT00434304 | GlaxoSmithKline |
Parkinson Disease
|
April 9, 2007 | Phase 2 |
| NCT00673088 | Roxane Laboratories|West-Ward Pharmaceutical |
Parkinson´s Disease|Restless Leg Syndrome
|
February 2004 | Not Applicable |
| NCT03708237 | University of Alberta |
Restless Legs Syndrome|End Stage Renal Disease
|
February 19, 2019 | Phase 2 |
| NCT03250117 | Titan Pharmaceuticals |
Parkinson Disease
|
October 10, 2017 | Phase 1|Phase 2 |
| NCT01627847 | Dr. Reddy´s Laboratories Limited |
Healthy
|
October 2009 | Phase 1 |
| NCT01627834 | Dr. Reddy´s Laboratories Limited |
Healthy
|
October 2009 | Phase 1 |
| NCT00221390 | University of California, Irvine|GlaxoSmithKline |
Cerebrovascular Accident|Hemiparesis
|
October 2003 | Phase 2 |
| NCT01628926 | Otsuka Pharmaceutical Co., Ltd. |
Parkinson´s Disease
|
June 2009 | Phase 3 |
| NCT00460148 | GlaxoSmithKline |
Parkinson Disease
|
April 2007 | Phase 2 |
| NCT00363857 | GlaxoSmithKline |
Restless Legs Syndrome (RLS)|Restless Legs Syndrome
|
August 2003 | Phase 3 |
| NCT00314860 | GlaxoSmithKline |
Restless Legs Syndrome|Restless Legs Syndrome (RLS)
|
February 2006 | Phase 3 |
| NCT00355641 | GlaxoSmithKline |
Restless Legs Syndrome
|
October 2005 | Phase 3 |
| NCT00419692 | GlaxoSmithKline |
Restless Legs Syndrome
|
August 24, 2006 | Phase 1 |
| NCT03176966 | Vanderbilt University Medical Center |
Muscle Cramp|Cirrhosis
|
September 2, 2016 | Phase 4 |
| NCT03038308 | Columbia University|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
Hyperprolactinemia|Prolactinoma
|
September 16, 2016 | Phase 1|Phase 2 |
| NCT00373542 | GlaxoSmithKline |
Restless Legs Syndrome (RLS)|Restless Legs Syndrome
|
October 2006 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 336.88 mM ; Need ultrasonic)
DMSO : 16.67 mg/mL ( 56.16 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3688 mL | 16.8441 mL | 33.6882 mL |
| 5 mM | 0.6738 mL | 3.3688 mL | 6.7376 mL |
| 10 mM | 0.3369 mL | 1.6844 mL | 3.3688 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (336.88 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (5.63 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.67 mg/mL (5.63 mM); Clear solution
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] Mavrikaki M, et al. Ropinirole regulates emotionality and neuronal activity markers in the limbic forebrain. Int J Neuropsychopharmacol. 2014 Dec;17(12):1981-93.
Synonyms