Novel and potent human and rat β3-Adrenergic receptor agonists containing substituted 3-indolylalkylamines
| Autor: | Shiro Kato, Hiroshi Harada, Naoyuki Yoshida, Yoshimi Hirokawa, Yasuji Furutani, Kenji Suzuki, Yoichi Hiyama, Hitoshi Kawashima, Mayumi Oue |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Models
Molecular Agonist Indoles medicine.drug_class Clinical Biochemistry Molecular Conformation Pharmaceutical Science Adrenergic beta-3 Receptor Agonists CHO Cells Pharmacology Biochemistry Chemical synthesis Structure-Activity Relationship Cricetinae Alkanes Drug Discovery Cyclic AMP medicine Animals Humans Structure–activity relationship Cloning Molecular Beta (finance) Molecular Biology Bicyclic molecule Chemistry Chinese hamster ovary cell Organic Chemistry Adrenergic beta-Agonists Tryptamines In vitro Rats Ethanolamines Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 13:1301-1305 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(03)00073-8 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect