Name | Rotigotine |
Synonyms | Neupro N 0923 SPM 962 Rotigotine (S)-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol [S,(-)]-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol ()-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-napht hol (-)-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-naphthol (6S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenol (6S)-6-{propyl[2-(thiophen-2-yl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol [2S,(-)]-N-Propyl-N-[2-(2-thienyl)ethyl]-5-hydroxy-1,2,3,4-tetrahydro-2β-naphthalenamine |
CAS | 99755-59-6 |
InChI | InChI=1/C19H25NOS/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21/h3-7,13,16,21H,2,8-12,14H2,1H3/t16-/m0/s1 |
Molecular Formula | C19H25NOS |
Molar Mass | 315.47 |
Density | 1.15±0.1 g/cm3(Predicted) |
Melting Point | 78 °C |
Boling Point | 470.1±45.0 °C(Predicted) |
Flash Point | 238.1°C |
Water Solubility | Insoluble in water |
Vapor Presure | 1.84E-09mmHg at 25°C |
Appearance | powder to crystal |
Color | White to Almost white |
pKa | 10.49±0.40(Predicted) |
Storage Condition | room temp |
Refractive Index | 1.611 |
MDL | MFCD00906149 |
Use | Rotigotine is a dopamine receptor agonist used in the treatment of Parkinson's disease and restless legs syndrome. |
In vitro study | Rotigotine (N-0437; N-0923) has a 10-fold selectivity for D3 (pK i 9.2) receptors compared with D2, D4 and D5 (pK i 8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK i 7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC 50 respectively: 9.0, 9.4-8.6, 9.7). Rotigotine (10 µM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 µM) slightly protects dopaminergic neurons against MPP + toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone. |
In vivo study | In primed rats, Rotigotine (N-0437; N-0923; 0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
HS Code | 2934990002 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.17 ml | 15.849 ml | 31.699 ml |
5 mM | 0.634 ml | 3.17 ml | 6.34 ml |
10 mM | 0.317 ml | 1.585 ml | 3.17 ml |
5 mM | 0.063 ml | 0.317 ml | 0.634 ml |