A New 5-HT3 Receptor Ligand. II. Structure-Activity Analysis of 5-HT3 Receptor Agonist Action in the Gut.
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چکیده
منابع مشابه
Menthol inhibits 5-HT3 receptor-mediated currents.
The effects of alcohol monoterpene menthol, a major active ingredient of the peppermint plant, were tested on the function of human 5-hydroxytryptamine type 3 (5-HT3) receptors expressed in Xenopus laevis oocytes. 5-HT (1 μM)-evoked currents recorded by two-electrode voltage-clamp technique were reversibly inhibited by menthol in a concentration-dependent (IC50 = 163 μM) manner. The effects of ...
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Our recently solved high-resolution structure of the serotonin 5-HT3 receptor (5-HT3R) delivered the first detailed structural insights for a mammalian pentameric ligand-gated ion channel. Based on this structure, we here performed a total of 2.8-μs all-atom molecular dynamics simulations to unravel at atomic detail how neurotransmitter binding on the extracellular domain induces sequential con...
متن کاملThe 5-HT3 receptor as a therapeutic target.
The 5-HT3 receptor is a neurotransmitter-gated ion channel. It is a member of the Cys-loop family of receptors, which also includes nicotinic acetylcholine, glycine and GABAA receptors. Each member of the family consists of an arrangement of five subunits surrounding a central ion-conducting pore. The 5-HT3 receptor binding site is composed of six loops from two adjacent subunits, and the criti...
متن کاملVarenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP
Cys-loop receptors are the site of action of many therapeutic drugs. One of these is the smoking cessation agent varenicline, which has its major therapeutic effects at nicotinic acetylcholine (nACh) receptors but also acts at 5-HT3 receptors. Here, we report the X-ray crystal structure of the 5-HT binding protein (5-HTBP) in complex with varenicline, and test the predicted interactions by prob...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 1998
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.46.445