Document Detail


Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.
MedLine Citation:
PMID:  12657269     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanols was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human beta(3)-AR. The optically active 30a was found to be the most potent and selective human beta(3)-AR agonist in this series with an EC(50) value of 0.062nM. In addition, 30a selectivity for human beta(3)-AR was 210-fold and 103-fold that for human beta(2)-AR and beta(1)-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat beta(3)-AR.
Authors:
Hiroshi Harada; Yoshimi Hirokawa; Kenji Suzuki; Yoichi Hiyama; Mayumi Oue; Hitoshi Kawashima; Naoyuki Yoshida; Yasuji Furutani; Shiro Kato
Related Documents :
21787789 - Crystal structure of crotoxin reveals key residues involved in the stability and toxici...
2876709 - Heterogeneity between soluble human and rabbit splenic alpha 2-adrenoceptors.
23446429 - Regulation of kallikrein-related peptidases in the skin - from physiology to diseases t...
21734189 - Residues 248-252 and 300-304 of the cardiac na+/ca2+ exchanger are involved in its regu...
6855479 - Lipid deterioration: beta-carotene destruction and oxygen evolution in a system contain...
11937059 - The structural basis for catalysis and specificity of the pseudomonas cellulosa alpha-g...
1825179 - Requirement for the beta,gamma-pyrophosphate bond of atp in a stage between transcripti...
11701129 - Crystal structure of a procaspase-7 zymogen: mechanisms of activation and substrate bin...
19282279 - Biochemical characterization and membrane topology of alg2 from saccharomyces cerevisia...
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  13     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2003 Apr 
Date Detail:
Created Date:  2003-03-26     Completed Date:  2003-11-03     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1301-5     Citation Subset:  IM    
Affiliation:
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki, Suita, Japan. hiroshi-harada@dainippon-pharm.co.jp
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Adrenergic beta-Agonists / chemical synthesis*,  pharmacology*
Alkanes / chemical synthesis*,  pharmacology*
Animals
CHO Cells
Cloning, Molecular
Cricetinae
Cyclic AMP / metabolism
Ethanolamines / pharmacology
Humans
Indoles / pharmacology*
Models, Molecular
Molecular Conformation
Rats
Receptors, Adrenergic, beta-3 / agonists*
Structure-Activity Relationship
Tryptamines / chemical synthesis,  pharmacology
Chemical
Reg. No./Substance:
0/Adrenergic beta-Agonists; 0/Alkanes; 0/Ethanolamines; 0/Indoles; 0/Receptors, Adrenergic, beta-3; 0/Tryptamines; 114333-71-0/BRL 37344; 60-92-4/Cyclic AMP

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.
Next Document:  Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2...