MT1 and MT2 Melatonin Receptors: A Therapeutic Perspective

J Liu, SJ Clough, AJ Hutchinson… - Annual review of …, 2016 - annualreviews.org
Melatonin, or 5-methoxy-N-acetyltryptamine, is synthesized and released by the pineal
gland and locally in the retina following a circadian rhythm, with low levels during the day …

Melatonin receptors: molecular pharmacology and signalling in the context of system bias

E Cecon, A Oishi, R Jockers - British journal of pharmacology, 2018 - Wiley Online Library
Melatonin, N‐acetyl‐5‐methoxytryptamine, an evolutionally old molecule, is produced by the
pineal gland in vertebrates, and it binds with high affinity to melatonin receptors, which are …

Synthesis and Structure−Affinity−Activity Relationships of Novel Benzofuran Derivatives as MT2 Melatonin Receptor Selective Ligands

V Wallez, S Durieux-Poissonnier… - Journal of medicinal …, 2002 - ACS Publications
A series of N-(2-phenylbenzofuran-3-yl) ethyl amide and N-(2-arylalkylbenzofuran-3-yl) ethyl
amide derivatives were synthesized and evaluated as melatonin receptor ligands. The …

Tetrahydroquinoline ring as a versatile bioisostere of tetralin for melatonin receptor ligands

S Rivara, L Scalvini, A Lodola, M Mor… - Journal of Medicinal …, 2018 - ACS Publications
A new family of melatonin receptor ligands, characterized by a tetrahydroquinoline (THQ)
scaffold carrying an amide chain in position 3, was devised as conformationally constrained …

Design and validation of the first family of photo-activatable ligands for melatonin receptors

G Somalo-Barranco, C Serra, D Lyons… - Journal of medicinal …, 2022 - ACS Publications
Melatonin is a neurohormone released in a circadian manner with peak levels at night.
Melatonin mediates its effects mainly through G protein-coupled MT1 and MT2 receptors …

Pharmacological actions of carbamate insecticides at mammalian melatonin receptors

GC Glatfelter, AJ Jones, RV Rajnarayanan… - … of Pharmacology and …, 2021 - ASPET
Integrated in silico chemical clustering and melatonin receptor molecular modeling
combined with in vitro 2-[125I]-iodomelatonin competition binding were used to identify …

High-throughput screening assay for new ligands at human melatonin receptors

J Yan, H Su, JA Boutin, MP Renard… - Acta Pharmacologica …, 2008 - nature.com
Aim: Melatonin (MT) is a neurohormone produced and secreted primarily by the pineal
gland in a circadian manner, and mainly acts through 2 receptor subtypes: MT 1 and MT 2 in …

Melatonin.

M Mor, PV Plazzi, G Spadoni… - Current medicinal …, 1999 - europepmc.org
Melatonin is the principal hormone secreted by the pineal gland, produced in humans with a
circadian rhythm characterized by elevated blood levels during the night. It is involved in the …

[HTML][HTML] Molecular characterization and pharmacology of melatonin receptors in animals

E Cecon, JA Boutin, R Jockers - Receptors, 2023 - mdpi.com
Melatonin, the hormone of darkness, is secreted in minute amounts during the night and is
virtually undetectable during the day. Melatonin mainly acts on high-affinity G protein …

Binding and unbinding of potent melatonin receptor ligands: Mechanistic simulations and experimental evidence

A Bedini, GM Elisi, F Fanini, M Retini… - Journal of Pineal …, 2024 - Wiley Online Library
The labeled ligand commonly employed in competition binding studies for melatonin
receptor ligands, 2‐[125I] iodomelatonin, showed slow dissociation with different half‐lives …