1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
Synonym(s):1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(3-(morpholin-4-yl)ethyl)-1H-indole hydrochloride;L768;ML-SI1 hydrochloride
- CAS NO.:180002-83-9
- Empirical Formula: C23H24Cl2N2O3
- Molecular Weight: 447.35
- MDL number: MFCD08061200
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-08 09:02:46
What is 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE?
The Uses of 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
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.
What are the applications of Application
GW-405833 is a CB2 partial agonist
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.
Properties of 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
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 |
Safety information for 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral H413:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P273:Avoid release to the environment. |
Computed Descriptors for 1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE
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