180002-83-9 Usage
Uses
Used in Pharmaceutical Industry:
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE is used as a potent and selective CB2 receptor partial agonist for the development of novel therapeutic agents targeting pain management and other related conditions. Its high affinity and selectivity for the CB2 receptor, along with its potent antihyperalgesic effects in rodent models, make it a valuable compound for the treatment of chronic and neuropathic pain.
Used in Pain Management:
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE is used as an analgesic agent for the management of various types of pain, including inflammatory, neuropathic, and chronic pain conditions. Its ability to produce potent antihyperalgesic effects in several rodent models of pain highlights its potential as a novel therapeutic agent for pain relief.
Used in Drug Discovery and Development:
1-(2,3-DICHLOROBENZOYL)-5-METHOXY-2-METHYL-3-[2-(4-MORPHOLINYL)ETHYL]-1H-INDOLE is used as a lead compound in drug discovery and development programs aimed at identifying and optimizing new therapeutic agents targeting the CB2 receptor. Its unique molecular structure and high affinity for the CB2 receptor make it an attractive starting point for the design and synthesis of novel CB2 receptor modulators with improved pharmacological properties and therapeutic potential.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 180002-83-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,0,0,0 and 2 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 180002-83:
(8*1)+(7*8)+(6*0)+(5*0)+(4*0)+(3*2)+(2*8)+(1*3)=89
89 % 10 = 9
So 180002-83-9 is a valid CAS Registry Number.
InChI:InChI=1/C23H24Cl2N2O3/c1-15-17(8-9-26-10-12-30-13-11-26)19-14-16(29-2)6-7-21(19)27(15)23(28)18-4-3-5-20(24)22(18)25/h3-7,14H,8-13H2,1-2H3
180002-83-9Relevant articles and documents
New class of potent ligands for the human peripheral cannabinoid receptor
Gallant, Michel,Dufresne, Claude,Gareau, Yves,Guay, Daniel,Leblanc, Yves,Prasit, Petpiboon,Rochette, Chantal,Sawyer, Nicole,Slipetz, Deborah M.,Tremblay, Nathalie,Metters, Kathleen M.,Labelle, Marc
, p. 2263 - 2268 (2007/10/03)
A new class of potent ligand for the human peripheral cannabinoid (hCB2) receptor is described. Two indole analogs 13 and 17 exhibited nanomolar potencies (K(i)) with good selectivity for the hCB2 receptor over the human central cannabinoid (hCB1) receptor.
Indole derivatives with affinity for the cannabinoid receptor
-
, (2008/06/13)
Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating glaucoma because of the activity on the cannabinoid recepto
