1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE Basic information
- Product Name:
- 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
- Synonyms:
-
- GW 405833
- (2,3-DICHLORO-PHENYL)-[5-METHOXY-2-METHYL-3-(2-MORPHOLIN-4-YL-ETHYL)-INDOL-1-YL]-METHANONE
- 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
- (2,3-DICHLORO-PHENYL)-[5-METHOXY-2-METHYL-3-(2-MORPHOLIN-4-YL-ETHYL)-INDOL-1-YL]-METHAN
- 1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(3-(morpholin-4-yl)ethyl)-1H-indole hydrochloride
- GW405833 hydrochloride
- (2,3-Dichloro-phenyl)-[5-Methoxy-2-Methyl-3-(2-Morpholin-4-yl-ethyl)-indol-1-yl]
- Methanone,(2,3-dichlorophenyl)[5-methoxy-2-methyl-3-[2-(4-morpholinyl)ethyl]-1H-indol-1-yl]-
- CAS:
- 180002-83-9
- MF:
- C23H24Cl2N2O3
- MW:
- 447.35
- Mol File:
- 180002-83-9.mol
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE Chemical Properties
- Melting point:
- 47-49℃
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO at 10-15mg/ml. Also soluble in ethanol at ~5mg/ml.
- form
- solid
- color
- tan
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE Usage And Synthesis
Uses
It is a potent and selective CB2 receptor partial agonist (EC50 = 0.65 nM; maximum inhibition = 44.6%). Binds with high affinity to both human and rat CB2 receptors and displays ~ 1200-fold selectivity over CB1 (Ki values are 3.92 and 4772 nM for human recombinant CB2 and CB1 receptors respectively). Produces potent antihyperalgesic effects in several rodent models of pain.
Definition
ChEBI: (2,3-dichlorophenyl)-[5-methoxy-2-methyl-3-[2-(4-morpholinyl)ethyl]-1-indolyl]methanone is a N-acylindole.
Biological Activity
Potent and selective CB 2 receptor partial agonist (EC 50 = 0.65 nM; maximum inhibition = 44.6%). Binds with high affinity to both human and rat CB 2 receptors and displays ~ 1200-fold selectivity over CB 1 (K i values are 3.92 and 4772 nM for human recombinant CB 2 and CB 1 receptors respectively). Produces potent antihyperalgesic effects in several rodent models of pain.
Biochem/physiol Actions
GW405833 is a selective cannabanoid CB2 receptor agonist; analgesic. GW405833 binds with high affinity at both human and rat CB2 receptors (Ki′s 3.9 and 3.6 nM); acts as a partial agonist (50% inhibition of forskolin-stimulated cAMP formation compared to full agonist CP55,940). GW405833 has potent analgesic activity in rat models of inflammatory, neuropathic and incisional pain; devoid of CNS effects common with CB1 agonists.
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLESupplier
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