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 …
its multiple roles mainly through two seven transmembrane domain, G-coupled receptors …
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 …
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 …
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 …
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
The MT2‐selective melatonin receptor ligand UCM765 (N‐(2‐((3‐methoxyphenyl)(phenyl)
amino) ethyl) acetamide), showed interesting sleep inducing, analgesic and anxiolytic …
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 …
machine (GS-SVM) and projection pursuit regression (PPR) were used to develop …
Designing multi-target drugs for the treatment of major depressive disorder
Introduction Major depressive disorders (MDD) pose major health burdens globally.
Currently available medications have their limitations due to serious adverse effects, long …
Currently available medications have their limitations due to serious adverse effects, long …
Design and validation of the first cell‐impermeant melatonin receptor agonist
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 …
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 …
synthesised by combinatorial chemistry using the mix and split method in the solid phase. A …