| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1359951 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,