New selective ligands of human cloned melatonin MT1 and MT2 receptors

V Audinot, F Mailliet, C Lahaye-Brasseur… - Naunyn-Schmiedeberg's …, 2003 - Springer
Melatonin has a key role in the circadian rhythm relay to periphery organs. Melatonin exerts
its multiple roles mainly through two seven transmembrane domain, G-coupled receptors …

Melatonin: functions and ligands

M Singh, HR Jadhav - Drug discovery today, 2014 - Elsevier
Highlights•Pathways controlling melatonin secretion are complex.•There are various causes
of melatonin disturbance.•Evaluation of melatonin secretion clinically requires long time …

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 …

Synthesis of substituted N-[3-(3-methoxyphenyl) propyl] amides as highly potent MT2-selective melatonin ligands

Y Hu, MKC Ho, KH Chan, DC New, YH Wong - Bioorganic & Medicinal …, 2010 - Elsevier
A series of substituted N-[3-(3-methoxyphenyl) propyl] amides were synthesized and their
binding affinities towards human melatonin MT1 and MT2 receptors were evaluated. It was …

Update on melatonin receptors: IUPHAR Review 20

R Jockers, P Delagrange… - British journal of …, 2016 - Wiley Online Library
Melatonin receptors are seven transmembrane‐spanning proteins belonging to the GPCR
superfamily. In mammals, two melatonin receptor subtypes exist‐MT1 and MT2‐encoded by …

N‐(Anilinoethyl)amide Melatonergic Ligands with Improved Water Solubility and Metabolic Stability

F Ferlenghi, M Mari, G Gobbi, GM Elisi, M Mor… - …, 2021 - Wiley Online Library
The MT2‐selective melatonin receptor ligand UCM765 (N‐(2‐((3‐methoxyphenyl)(phenyl)
amino) ethyl) acetamide), showed interesting sleep inducing, analgesic and anxiolytic …

A novel quantitative structure–activity relationship method to predict the affinities of MT3 melatonin binding site

H Du, J Wang, X Zhang, Z Hu - European journal of medicinal chemistry, 2008 - Elsevier
The linear regression (LR) and non-linear regression methods–grid search-support vector
machine (GS-SVM) and projection pursuit regression (PPR) were used to develop …

Designing multi-target drugs for the treatment of major depressive disorder

AK Halder, S Mitra, MNDS Cordeiro - Expert Opinion on Drug …, 2023 - Taylor & Francis
Introduction Major depressive disorders (MDD) pose major health burdens globally.
Currently available medications have their limitations due to serious adverse effects, long …

Design and validation of the first cell‐impermeant melatonin receptor agonist

F Gbahou, E Cecon, G Viault, R Gerbier… - British journal of …, 2017 - Wiley Online Library
Background and Purpose The paradigm that GPCRs are able to prolong or initiate cellular
signalling through intracellular receptors recently emerged. Melatonin binds to G protein …

Synthesis of a small library of phenylalkylamide derivatives as melatoninergic ligands for human mt1 and MT2 receptors

C Pégurier, S Curtet, JP Nicolas, JA Boutin… - Bioorganic & medicinal …, 2000 - Elsevier
Focused small libraries of melatonin receptor ligands from arylalkylamine derivatives were
synthesised by combinatorial chemistry using the mix and split method in the solid phase. A …