| Chen CM |
------>authors3_c=None ------>paper_class1=1 ------>Impact_Factor=None ------>paper_class3=1 ------>paper_class2=1 ------>vol=43 ------>confirm_bywho=cmbyeh ------>insert_bywho=lai03 ------>Jurnal_Rank=None ------>authors4_c=None ------>comm_author= ------>patent_EDate=None ------>authors5_c=None ------>publish_day=1 ------>paper_class2Letter=None ------>page2=8 ------>medlineContent= ------>unit=E0113 ------>insert_date=20060215 ------>iam=3 ------>update_date=None ------>author=??? ------>change_event=4 ------>ISSN= ------>authors_c=None ------>score=-32 ------>journal_name=Acta Paediatrica Taiwanica ------>paper_name=Chang Position Dose Not Improve the Efficacy of Conventional Phototherapy ------>confirm_date=20060215 ------>tch_id=087023 ------>pmid=19530697 ------>page1=255 ------>fullAbstract=By using the active metabolite 5 as an initial template, further structural modifications led to the identification of the titled compound 24 (BPR-890) as a highly potent CB1 inverse agonist possessing an excellent CB2/1 selectivity and remarkable in vivo efficacy in diet-induced obese mice with a minimum effective dose as low as 0.03 mg/kg (po qd) at the end of the 30-day chronic study. Current SAR studies along with those of many existing rimonabant-mimicking molecules imply that around the pyrazole C3-position, a rigid and deep binding pocket should exist for CB1 receptor. In addition, relative to the conventional carboxamide carbonyl, serving as a key hydrogen-bond acceptor during ligand-CB1 receptor interaction, the corresponding polarizable thione carbonyl might play a more critical role in stabilizing the Asp366-Lys192 salt bridge in the proposed CB1-receptor homology model and inducing significant selectivity for CB1R over CB2R. ------>tmu_sno=None ------>sno=12896 ------>authors2=Liu SH ------>authors3=Lai CC ------>authors4=Hwang CC ------>authors5=Hsu HH ------>authors6= ------>authors6_c=None ------>authors=Chen CM ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c=None ------>publish_area=0 ------>updateTitle=Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1, 5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice. ------>language=2 ------>check_flag=None ------>submit_date=None ------>country=None ------>no=5 ------>patent_SDate=None ------>update_bywho=None ------>publish_year=2002 ------>submit_flag=None ------>publish_month=10 |