Design,synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors |
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| Authors: | Alessia Carocci Alessia Catalano Angelo Lovece Giovanni Lentini Andrea Duranti Valeria Lucini Marilou Pannacci Francesco Scaglione Carlo Franchini |
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| Institution: | 1. Dipartimento Farmaco-Chimico, Università degli Studi di Bari, Via E. Orabona 4, 70126 Bari, Italy;2. Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Urbino ‘Carlo Bo’, Piazza del Rinascimento 6, 61029 Urbino, Italy;3. Dipartimento di Farmacologia, Chemioterapia e Tossicologia Medica, Università degli Studi di Milano, Via Vanvitelli 32, 20129 Milano, Italy |
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| Abstract: | A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists. |
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