ROTIGOTINE
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- CAS-Nr.
- 99755-59-6
- Englisch Name:
- ROTIGOTINE
- Synonyma:
- Neupro;N 0923;CS-110;SPM 962;Rotigotine;S(-)-N-0437;14C]-Rotigotine;Rotigotine (Base);Rotigotine (N-0437;ROTIGOTINE USP/EP/BP
- CBNumber:
- CB81001679
- Summenformel:
- C19H25NOS
- Molgewicht:
- 315.47
- MOL-Datei:
- 99755-59-6.mol
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ROTIGOTINE Eigenschaften
- Schmelzpunkt:
- 78 °C
- Siedepunkt:
- 470.1±45.0 °C(Predicted)
- Dichte
- 1.15±0.1 g/cm3(Predicted)
- storage temp.
- room temp
- Wasserl?slichkeit
- Insoluble in water
- L?slichkeit
- DMF: 30 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 20 mg/ml; Ethanol: 1 mg/ml
- pka
- 10.49±0.40(Predicted)
- Aggregatzustand
- powder to crystal
- Farbe
- White to Almost white
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
 
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H336 |
Kann Schl?frigkeit und Benommenheit verursachen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Schl?frigkeit und Benommenheit) |
Warnung |
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P261, P271, P304+P340, P312,P403+P233, P405, P501 |
| H361 |
Kann vermutlich die Fruchtbarkeit beeintr?chtigen oder das Kind im Mutterleib sch?digen. |
Reproduktionstoxizit?t |
Kategorie 2 |
Warnung |
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P201, P202, P281, P308+P313, P405,P501 |
| H362 |
Kann S?uglinge über die Muttermilch sch?digen. |
Reproductive toxicity, effects on or via lactation |
Additional category |
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P201, P260, P263, P264, P270,P308+P313 |
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| Sicherheit |
| P201 |
Vor Gebrauch besondere Anweisungen einholen. |
| P202 |
Vor Gebrauch alle Sicherheitshinweise lesen und verstehen. |
| P260 |
Dampf/Aerosol/Nebel nicht einatmen. |
| P261 |
Einatmen von Staub vermeiden. |
| P263 |
Kontakt w?hrend der Schwangerschaft /und der Stillzeit vermeiden. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P271 |
Nur im Freien oder in gut belüfteten R?umen verwenden. |
| P281 |
Vorgeschriebene pers?nliche Schutzausrüstung verwenden. |
| P304+P340 |
BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen. |
| P308+P313 |
BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P312 |
Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
| P403+P233 |
An einem gut belüfteten Ort aufbewahren. Beh?lter dicht verschlossen halten. |
| P405 |
Unter Verschluss aufbewahren. |
| P501 |
Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen. |
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ROTIGOTINE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
While levodopa is still considered the cornerstone of treatment of Parkinson’s
disease, many patients begin to experience treatment-related problems, such as a
wearing-off phenomenon and the development of dyskinesias as the disease
progresses. Continuous dopaminergic stimulation by means of a dopamine
agonist has been recognized as being associated with a lower incidence of
dyskinesias. Using a selective dopamine agonist as monotherapy in early disease
may delay the onset of levodopa therapy, or at a minimum, lower its dose in
adjunctive situations to minimize the adverse neurotoxic effects of levodopa.
Rotigotine is a nonergolinic dopamine D3/D2/D1 receptor agonist, and it is the
first dopamine agonist to be launched as a transdermal patch.
Verwenden
It is a non-ergot dopamine agonist drug and is indicated for the treatment of Parkinson disease.
Allgemeine Beschreibung
Rotigotine, (6S)-6-{propyl[2-(2-thienyl)ethyl]amino}-5,6,7,8-tetrahydro-1-naphthalenol (Neupro),is a nonergoline that is available as a silicone-based, selfadhesivematrix, transdermal system for continuous delivery over a 24-hour period. Approximately 45% of the drug is releasedwithin 24 hours. The terminal half-life of rotigotine is5 to 7 hours after removal of the patch. Rotigotine is 90%bound to plasma proteins. The compound undergoes extensivemetabolism and has low bioavailability by the oralroute. The major metabolites of rotigotine are the glucuronideand sulfate conjugates of rotigotine and sulfateconjugates of N-despropylrotigotine and N-desthienylethylrotigotine. Rotigotine is excreted in the urine (71%) andfeces (11%).Studies using human liver microsomes didnot find any interactions with CYP1A2, CYP2C9,CYP2C19, CYP2D6, and CYP3A4 substrates.Rotigotinetransdermal system contains sodium metabisulfite, and individualssensitive to sulfite could be at risk for allergic reactions.Additionally, somnolence is a common adverse reactionwith individuals on rotigotine, and patients should beclosely monitored during therapy.In transfected Chinesehamster ovary (CHO) cells, rotigotine binds with high affinityat D
3 and D
2L receptors (variants in the D
2 receptor subtypeare caused by insertion of the 29 amino acids into thethird loop to give D
2s and D
2L).Using rat CHO cells,rotigotine shows over 30-fold selectivity at D3 versus D2 receptors.48 Rotigotine was approved in May 2007 for thetreatment of early-stage PD.
ROTIGOTINE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
2-Thiopheneethanamine, N-propyl-N-[(2S)-1,2,3,4-tetrahydro-5-methoxy-2-naphthalenyl]-, hydrobromide (1:1)
Benzenesulfonic acid, 4-nitro-, 2-(2-thienyl)ethyl ester
Benzenesulfonic acid, 2-nitro-, 2-(2-thienyl)ethyl ester
2-(2-Thienyl)ethyltoluol-p-sulfonat
5-Methoxy-2-tetralone
(S)-1,2,3,4-tetrahydro-5-methoxy-N-propyl-2-Naphthalenamine(Rotigotine)
Rotigotine Impurity 7
N-Propyl-N-[(2S)-1,2,3,4-tetrahydro-5-methoxy-2-naphthalenyl]-2-thiopheneethanamine hydrochloride
(6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride
(S)-5-Methoxy-N-propyl-N-(2-(thiophen-2-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-2-aMine
(-)-(6-PROPYLAMINO)-5,6,7,8-TETRAHYDRO-NAPHTHALEN-1-OL
2-Thienylessigsaeure
Downstream Produkte
ROTIGOTINE Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 262)Lieferanten
99755-59-6()Verwandte Suche:
- ()-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-napht hol
- (6S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenol
- N 0923
- SPM 962
- (S)-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol
- [2S,(-)]-N-Propyl-N-[2-(2-thienyl)ethyl]-5-hydroxy-1,2,3,4-tetrahydro-2β-naphthalenamine
- [S,(-)]-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol
- S(-)-N-0437
- Rotigotine
- 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-(6S)-1-naphthalenol
- (?)-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-naphthol hydrochloride
- (6S)-6-(Propyl(2-(2-thienyl)ethyl)amino)-5,6,7,8-tetrahydro-1-naphthalenol
- 1-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-, (6S)-
- CS-110
- (6S)-6-{propyl[2-(thiophen-2-yl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol
- Rotigotine (Base)
- ROTIGOTINE USP/EP/BP
- Rotigotine EP Impurity G
- Rotigotine (N-0437
- RotigotineQ: What is
Rotigotine Q: What is the CAS Number of
Rotigotine Q: What is the storage condition of
Rotigotine Q: What are the applications of
Rotigotine
- 1-a]isoquinolin-4-one
- 2-morpholino-4H-pyrimido[2
- Neupro
- 14C]-Rotigotine
- rotigotine impurities
- 99755-59-6
- C19H25NOS
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Sulfur & Selenium Compounds
