| Identification | Back Directory | [Name]
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE | [CAS]
169675-09-6 | [Synonyms]
RO 60-0175 FUMARATE
Ro 600175 fumarate,Ro 60 0175 fumarate
(S)-2-(Chloro-5-fluoro-indol-L-yl)-1-methylethylamine fumarate
(αS)-6-Chloro-5-fluoro-α-methyl-1H-indole-1-ethanaminefumarate
(S)-1-(6-Chloro-5-fluoro-1H-indol-1-yl)propan-2-amine fumarate
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
(alpha-S)-6-Chloro-5-fluoro-alpha-methyl-(1H)-indole-1-ethaneaminefumarate
1H-Indole-1-ethanaMine, 6-chloro-5-fluoro-a-Methyl-, (aS)-, (2E)-2-butenedioate
1H-Indole-1-ethanamine, 6-chloro-5-fluoro-alpha-methyl-, (S)-, (E)-2-butenedioate (1:1)
1H-Indole-1-ethanamine, 6-chloro-5-fluoro-alpha-methyl-, (alphas)-, (2E)-2-butenedioate (1:1) | [Molecular Formula]
C15H16ClFN2O4 | [MDL Number]
MFCD06798313 | [MOL File]
169675-09-6.mol | [Molecular Weight]
342.75 |
| Hazard Information | Back Directory | [Description]
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively). It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 or the 5-HT2A antagonist MDL 100,907 (volinanserin; ). | [Uses]
Ro 60-0175 fumarate is a potent and selective SR-2 agonist. | [Biological Activity]
Potent, selective 5-HT 2 receptor agonist; shows selectivity for the 5-HT 2C subtype (pK i values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT 2C , 2A , 1A , 6 and 7 receptors respectively). Centrally active following oral or systemic administration in vivo . | [in vivo]
Ro60-0175 (1 mg/kg; s.c.) fumarate 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 (Ro60-0175); 1?mg/kg (yohimbine); s.c.; i.p.) fumarate dose dependently attenuates the response increased by the yohimbine treatment alone relative to vehicle injection[1].
Ro60-0175 (0.5 mg/kg (SB242084); 1?mg/kg (Ro60-0175); 1?mg/kg (yohimbine); s.c.; i.p.) fumarate reduces responding and that this effect is prevented by SB242084 pretreatment[1].
Ro60-0175 (0.3, 1, and?3 mg/kg; s.c.) fumarate 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.) fumarate 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]. | [IC 50]
5-HT2C Receptor | [storage]
Desiccate at RT | [References]
[1] R H P PORTER. Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells[J]. British Journal of Pharmacology, 2009, 128 1: 13-20. DOI: 10.1038/sj.bjp.0702751
[2] J R MARTIN. 5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 286 2: 913-924.
[3] K J DAMJANOSKA. Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol- l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine(2C) receptor agonist.[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 304 3: 1209-1216. DOI: 10.1124/jpet.102.043489 |
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