China
Africa
Explore chapters and articles related to this topic
Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Piromelatine known as Neu-P11 is a newer melatonin receptor agonist underdevelopmental stage. It acts on MT1, MT2, and also 5-HT1A/5-HT1D receptors. It has demonstrated improvement in the sleep cycle of primary insomnia patients and reducing sleep disturbances in Phase II clinical trial. It was found to have efficacy in maintaining deeper sleep, less arousal, and also preserving REM sleep pattern. In the clinical trial, piromelatine was well tolerated with no adverse effects on psychomotor performance the following day (She et al., 2014).
In silico drug discovery of melatonin receptor ligands with therapeutic potential
Published in Expert Opinion on Drug Discovery, 2022
Gian Marco Elisi, Laura Scalvini, Alessio Lodola, Annalida Bedini, Gilberto Spadoni, Silvia Rivara
Unfortunately, only a few of these compounds have progressed to a thorough pharmacological characterization, to in vivo studies, and very few to clinical trials (e.g., piromelatine [87] and beta-methyl-6-chloromelatonin [88] in addition to the approved agonists). Nevertheless, some compounds, in particular subtype-selective ligands, have been successfully used to clarify the role of melatonergic receptors in certain tissues or processes, as happened, for example, with IIK7 and UCM765 in sleep induction and maintenance. Melatonergic ligands designed through a ligand-based approach have chemical structures reminiscent of that of melatonin, usually comprising an aromatic scaffold, an amide group, and a hydrogen bond acceptor mimicking the methoxy group, combined in such a way to mimic the steric and conformational properties of the natural ligand. For these compounds, we can expect an arrangement at the ligand binding site and interactions with receptor residues consistent with those of melatonin.