| Identification | Back Directory | [Name]
Ro 60-0175 | [CAS]
169675-08-5 | [Synonyms]
Ro 60-0175
1H-Indole-1-ethanamine, 6-chloro-5-fluoro-α-methyl-, (αS)-
(aS)-6-Chloro-5-fluoro-a-methyl-1H-indole-1-ethanamine monofumarate
selective,cocaine,Inhibitor,Ro600175,contextual cues,inhibit,yohimbine,5-hydroxytryptamine Receptor,5-HT2C,Ro60 0175,Ro-60-0175,drug-seeking,self-administration,5-HT Receptor,Serotonin Receptor | [Molecular Formula]
C11H12ClFN2 | [MDL Number]
MFCD06798313 | [MOL File]
169675-08-5.mol | [Molecular Weight]
226.68 |
| Chemical Properties | Back Directory | [Boiling point ]
353.2±32.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO : 125 mg/mL (551.44 mM; Need ultrasonic) | [form ]
Solid | [pka]
9.58±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Ro60-0175 is a potent and selective agonist of 5-HT2C receptor. Ro60-0175 reduces self-administration[1]. | [Definition]
ChEBI: (2S)-1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine is a 1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine that has S configuration. A selective agonist for both the 5-hydroxytryptamine 2B (5-HT2B) and 5-hydroxytryptamine 2C (5-HT2C)serotonin receptor subtypes, commonly used as fumarate salt. It has a role as a 5-hydroxytryptamine 2B receptor agonist and a 5-hydroxytryptamine 2C receptor agonist. | [in vivo]
Ro60-0175 (1 mg/kg; s.c.) preserves the regularity of responding seen in control animals in drug-treated group, but drug-treated animals reach their break-points earlier[1].
Ro60-0175 (0.3, 1, and 3 mg/kg; s.c.) significantly reduces responding on the active lever in the reinstatement group[1].
Ro60-0175 (0.5 mg/kg SB242084; 1 mg/kg Ro60-0175; s.c.; i.p.) reduces responding compared to vehicle in the reinstatement group, and that this effect is prevented by pretreatment with SB242084. For responding on the inactive lever, there are no significant main effects or interactions[1]. | Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | | Dosage: | 1 mg/kg | | Administration: | s.c. | | Result: | Preserved the regularity of responding seen in control animals in drug-treated group, but drug-treated animals reached their break-points earlier. |
| Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | | Dosage: | 0.5?mg/kg (SB242084), 1?mg/kg (Ro60-0175) | | Administration: | s.c. (Ro60-0175), i.p. (SB242084) | | Result: | Reduced responding for cocaine and effect was reversed by SB242084. |
| Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | | Dosage: | 0.3, 1, and?3 mg/kg (Ro60-0175), 1?mg/kg (yohimbine) | | Administration: | s.c. (Ro60-0175), i.p. (yohimbine) | | Result: | Showed yohimbine treatment alone increased responding relative to vehicle injection, and the response was attenuated dose dependently by Ro60-0175. |
| Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | | Dosage: | 0.5 mg/kg (SB242084), 1?mg/kg (Ro60-0175), 1?mg/kg (yohimbine) | | Administration: | s.c. (Ro60-0175), i.p. (yohimbine), i.p. (SB242084) | | Result: | Ro60-0175 reduced responding and that this effect was prevented by SB242084 pretreatment. |
| [IC 50]
5-HT2C Receptor | [References]
[1] Fletcher PJ, et al. The 5-HT2C receptor agonist Ro60-0175 reduces cocaine self-administration and reinstatement induced by the stressor yohimbine, and contextual cues. Neuropsychopharmacology. 2008;33(6):1402-1412. DOI:10.1038/sj.npp.1301509 |
|
|