Document Detail

Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.
MedLine Citation:
PMID:  12657269     Owner:  NLM     Status:  MEDLINE    
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.
Hiroshi Harada; Yoshimi Hirokawa; Kenji Suzuki; Yoichi Hiyama; Mayumi Oue; Hitoshi Kawashima; Naoyuki Yoshida; Yasuji Furutani; Shiro Kato
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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    
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki, Suita, Japan.
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MeSH Terms
Adrenergic beta-Agonists / chemical synthesis*,  pharmacology*
Alkanes / chemical synthesis*,  pharmacology*
CHO Cells
Cloning, Molecular
Cyclic AMP / metabolism
Ethanolamines / pharmacology
Indoles / pharmacology*
Models, Molecular
Molecular Conformation
Receptors, Adrenergic, beta-3 / agonists*
Structure-Activity Relationship
Tryptamines / chemical synthesis,  pharmacology
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

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