(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE Basic information
- Product Name:
- (AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
- Synonyms:
-
- RO 60-0175 FUMARATE
- 1H-Indole-1-ethanaMine, 6-chloro-5-fluoro-a-Methyl-, (aS)-, (2E)-2-butenedioate
- (AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
- (alpha-S)-6-Chloro-5-fluoro-alpha-methyl-(1H)-indole-1-ethaneaminefumarate
- (S)-2-(Chloro-5-fluoro-indol-L-yl)-1-methylethylamine fumarate
- 1H-Indole-1-ethanamine, 6-chloro-5-fluoro-alpha-methyl-, (alphas)-, (2E)-2-butenedioate (1:1)
- 1H-Indole-1-ethanamine, 6-chloro-5-fluoro-alpha-methyl-, (S)-, (E)-2-butenedioate (1:1)
- (αS)-6-Chloro-5-fluoro-α-methyl-1H-indole-1-ethanaminefumarate
- CAS:
- 169675-09-6
- MF:
- C15H16ClFN2O4
- MW:
- 342.75
- Mol File:
- 169675-09-6.mol
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE Chemical Properties
- storage temp.
- Desiccate at RT
- solubility
- Soluble to 5 mM in water and to 20 mM in DMSO
- form
- Powder
- color
- White to off-white
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE Usage And Synthesis
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 .
storage
Desiccate at RT
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATESupplier
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