N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist

N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide 3a was synthesized as an orally bioavailable agonist at MT1 and MT2 melatonin receptors with significantly low vasoconstrictive activity.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-10, Vol.14 (20), p.5157
Main Authors: Sun, Li-Qiang, Takaki, Katherine, Chen, Jie, Iben, Lawrence, Knipe, Jay O, Pajor, Lori, Mahle, Cathy D, Ryan, Elaine, Xu, Cen
Format: Article
Language:English
Subjects:
Acetamides - chemical synthesis
Acetamides - pharmacokinetics
Acetamides - toxicity
Administration, Oral
Animals
Benzofurans - chemical synthesis
Benzofurans - pharmacokinetics
Benzofurans - toxicity
Biological Availability
Cyclic AMP - antagonists & inhibitors
Cyclic AMP - biosynthesis
Dose-Response Relationship, Drug
Humans
In Vitro Techniques
Mice
Muscle Contraction - drug effects
Muscle, Smooth, Vascular - drug effects
Muscle, Smooth, Vascular - physiology
NIH 3T3 Cells
Radioligand Assay
Rats
Receptor, Melatonin, MT1 - agonists
Receptor, Melatonin, MT2 - agonists
Structure-Activity Relationship
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Description
Summary:N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide 3a was synthesized as an orally bioavailable agonist at MT1 and MT2 melatonin receptors with significantly low vasoconstrictive activity.
ISSN:0960-894X
1464-3405