3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDE
3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDE Basic information
- Product Name:
- 3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDE
- Synonyms:
-
- 3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDE
- GR 46611
- 3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]prop-2-enamide
- 2-Propenamide, 3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]-
- GR 46611, 5-HT1B/1D agonist
- CAS:
- 185259-85-2
- MF:
- C23H27N3O2
- MW:
- 377.48
- Mol File:
- 185259-85-2.mol
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3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDE Chemical Properties
- Boiling point:
- 645.9±55.0 °C(Predicted)
- Density
- 1.168
- storage temp.
- 2-8°C
- solubility
- DMSO: 28 mg/mL, soluble
- pka
- 14.51±0.46(Predicted)
- form
- solid
- color
- white
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MSDS
- Language:English Provider:SigmaAldrich
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3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDE Usage And Synthesis
Uses
GR 46611is a 5-HT1D agonist.
Definition
ChEBI: 3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]-2-propenamide is a member of tryptamines.
Biological Activity
5-HT 1D receptor agonist. Blockade of GR 46611-induced hypothermia in the guinea pig provides a useful model with which to study the potency and duration of action of centrally acting 5-HT 1D receptor ligands.
in vivo
GR-46611 (1 mg/kg, i.p. ) significantly improves survival of Dravet syndrome (DS) mice[1].
GR-46611 (0.03-300 μg/kg, i.v.) increases threshold volume, bladder capacity, and residual volume in chronic spinal cord injury (SCI) cats[3].
GR46611 (3-30 mg/kg, s.c.) causes a dose-related decrease in rectal temperature in the adult guinea-pig[4].
| Animal Model: | Dravet syndrome (DS) mice[1] |
| Dosage: | 0.01, 0.1 and 1 mg/kg |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Improved survival relative to vehicle treated controls with 89% surviving rate. |
IC 50
5-HT1D Receptor
3-[3-(2-DIMETHYLAMINOETHYL)-1H-INDOL-5-YL]-N-(4-METHOXYBENZYL)ACRYLAMIDESupplier
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