Drugs for insomnia beyond benzodiazepines: pharmacology, clinical applications, and discovery

T Atkin, S Comai, G Gobbi - Pharmacological reviews, 2018 - ASPET
Although the GABAergic benzodiazepines (BZDs) and Z-drugs (zolpidem, zopiclone, and
zaleplon) are FDA-approved for insomnia disorders with a strong evidence base, they have …

CCNP Award Paper: Unveiling the role of melatonin MT2 receptors in sleep, anxiety and other neuropsychiatric diseases: a novel target in psychopharmacology

S Comai, G Gobbi - Journal of Psychiatry and Neuroscience, 2014 - jpn.ca
Background: Melatonin (MLT) is a pleiotropic neurohormone controlling many physiological
processes and whose dysfunction may contribute to several different diseases, such as …

[HTML][HTML] Melatonin in aging and disease—multiple consequences of reduced secretion, options and limits of treatment

R Hardeland - Aging and disease, 2012 - ncbi.nlm.nih.gov
Melatonin is a pleiotropically acting regulator molecule, which influences numerous
physiological functions. Its secretion by the pineal gland progressively declines by age …

Melatonin receptor ligands: a pharmaco‐chemical perspective

JA Boutin, PA Witt‐Enderby, C Sotriffer… - Journal of pineal …, 2020 - Wiley Online Library
Melatonin MT1 and MT2 receptor ligands have been vigorously explored for the last 4
decades. Inspection of approximately 80 publications in the field revealed that most …

Selective melatonin MT2 receptor ligands relieve neuropathic pain through modulation of brainstem descending antinociceptive pathways

M Lopez-Canul, E Palazzo, S Dominguez-Lopez… - Pain, 2015 - journals.lww.com
Neuropathic pain is an important public health problem for which only a few treatments are
available. Preclinical studies show that melatonin (MLT), a neurohormone acting on MT1 …

Melatonin receptor structure and signaling

HH Okamoto, E Cecon, O Nureki… - Journal of Pineal …, 2024 - Wiley Online Library
Abstract Melatonin (5‐methoxy‐N‐acetyltryptamine) binds with high affinity and specificity to
membrane receptors. Several receptor subtypes exist in different species, of which the …

The location, physiology, pathology of hippocampus Melatonin MT2 receptor and MT2-selective modulators

Y Feng, X Jiang, W Liu, H Lu - European Journal of Medicinal Chemistry, 2023 - Elsevier
Melatonin, a neurohormone secreted by the pineal gland and regulated by the
suprachiasmatic nucleus (SCN) of the hypothalamus, is synthesized and directly released …

Anxiolytic effects of the melatonin MT2 receptor partial agonist UCM765: Comparison with melatonin and diazepam

R Ochoa-Sanchez, Q Rainer, S Comai… - Progress in neuro …, 2012 - Elsevier
Melatonin (MLT) is a neurohormone known to be involved in the regulation of anxiety. Most
of the physiological actions of MLT in the brain are mediated by two high-affinity G-protein …

Synthesis of tryptamine derivatives via a direct, one-pot reductive alkylation of indoles

M Righi, F Topi, S Bartolucci, A Bedini… - The Journal of …, 2012 - ACS Publications
An efficient, one-pot reductive alkylation of indoles with N-protected aminoethyl acetals in
the presence of TES/TFA is reported. It represents the first general method for the direct …

Melatonin and synthetic melatonergic agonists: actions and metabolism in the central nervous system

R Hardeland, B Poeggeler - Central Nervous System Agents in …, 2012 - ingentaconnect.com
The CNS is both source and target of melatonin. This methoxyindole formed in the pineal
gland is also produced in other CNS regions and additionally enters the brain by uptake …