Study M1014
Study name | Zhang Y 2022b |
Title | Discovery of 1-(Hetero)aryl-beta-carboline derivatives as IDO1/TDO dual inhibitors with antidepressant activity |
Overall design | The aim of this study was to validate the possibility of targeting IDO1/TDO for inflammation-induced depression treatment. In this study, 1-(1H-Imidazole-5-yl)-9H-pyrido[3,4-b]indole was discovered as an IDO1/TDO dual inhibitor with antidepressant activity in the lipopolysaccharide induced depression model. C57BL/6J mice were divided into the following 3 groups (n = 8-10 in each group): (1) control group, (2) lipopolysaccharide group, and (3) lipopolysaccharide + 1-(1H-Imidazole-5-yl)-9H-pyrido[3,4-b]indole group. 1-(1H-Imidazole-5-yl)-9H-pyrido[3,4-b]indole (20 mg/kg/day) was administered once daily for 2 days, then lipopolysaccharide (2 mg/kg) was administered on the third day. The levels of kynurenine in the serum and brain were detected using the LC-MS. |
Study Type | Type1; Type2; |
Data available | Unavailable |
Organism | Mouse; C57BL/6J mouse; |
Categories of depression | Animal model; Lipopolysaccharide induced depression model; Lipopolysaccharide induced depression model; |
Criteria for depression | Forced swimming test, tail suspension test |
Sample size | 28 |
Tissue | Central; Brain; Brain; Peripheral; Blood; Serum; |
Platform | MS-based; LC-MS: Agilent 6500 time-of-flight liquid chromatography−mass spectrometry; |
PMID | |
DOI | |
Citation | Zhang Y, Li Y, Chen X, et al. Discovery of 1-(Hetero)aryl-beta-carboline derivatives as IDO1/TDO dual inhibitors with antidepressant activity. J Med Chem. 2022 Aug 25;65(16):11214-11228. |
Metabolite |
