کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1359951 | 981421 | 2013 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel highly potent serotonin 5-HT7 receptor ligands: Structural modifications to improve pharmacokinetic properties
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
Here we report the synthesis, pharmacological and pharmacokinetic evaluation of a pilot set of compounds structurally related to the potent and selective 5-HT7 ligand LP-211. Among the studied compounds, N-pyridin-3-ylmethyl-3-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]ethoxy]propanamide (4b) showed high affinity for 5-HT7 receptors (Ki = 23.8 nM), selectivity over 5-HT1A receptors (>50-fold), in vitro metabolic stability (82%) and weak interaction with P-glycoprotein (BA/AB = 3.3). Compound 4b was injected ip in mice to preliminarily evaluate its distribution between blood and brain.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 22, 15 November 2013, Pages 6083–6086
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 22, 15 November 2013, Pages 6083–6086
نویسندگان
Enza Lacivita, Pantaleo Di Pilato, Madia Letizia Stama, Nicola Antonio Colabufo, Francesco Berardi, Roberto Perrone, Bianca De Filippis, Giovanni Laviola, Walter Adriani, Mauro Niso, Marcello Leopoldo,