1202865-22-2
Chemical Structure
GW405833 hydrochloride
Synonym(s): L768242 hydrochloride
- CAS No.: 1202865-22-2
- Formula:C23H25Cl3N2O3
- Molecular Weight:483.82
IUPAC Name: (2,3-dichlorophenyl)(5-methoxy-2-methyl-3-(2-morpholinoethyl)-1H-indol-1-yl)methanone hydrochloride
InChIKey: JIQYDHDVNNFPMU-UHFFFAOYSA-N
SMILES: O=C(C1=C(C(Cl)=CC=C1)Cl)N2C3=C(C=C(OC)C=C3)C(CCN4CCOCC4)=C2C.Cl
Biological Activity: GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF)[1][2][3][4][5][6].
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GW405833 hydrochloride | 99.59% | GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF). | ||||||||||||||||||||
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- [1]. Li AL, Carey LM, Mackie K, Hohmann AG. Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther. 2017;362(2):296-305. [Content Brief]
- [2]. Li J, et al. Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation. Medchemcomm. 2019 Sep 17;10(11):1935-1947. [Content Brief]
- [3]. Parlar A, Arslan SO, Doğan MF, et al. The exogenous administration of CB2 specific agonist, GW405833, inhibits inflammation by reducing cytokine production and oxidative stress. Exp Ther Med. 2018;16(6):4900-4908. [Content Brief]
- [4]. Marini P, Cascio MG, King A, Pertwee RG, Ross RA. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol. 2013;169(4):887-899. [Content Brief]
- [5]. Cai SL, et al. CB2R agonist GW405833 alleviates acute liver failure in mice via inhibiting HIF-1α-mediated reprogramming of glycometabolism and macrophage proliferation. Acta Pharmacol Sin. 2023 Jul;44(7):1391-1403. [Content Brief]
- [6]. Valenzano KJ, et al. Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology. 2005 Apr;48(5):658-72. [Content Brief]
Keywords
