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HomeProduct name list1-(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

Synonym(s):1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(3-(morpholin-4-yl)ethyl)-1H-indole hydrochloride;L768;ML-SI1 hydrochloride

1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE Structural

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)
ghs
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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