Tetrahydronaphthalenic derivatives as new agonist and antagonist ligands for melatonin receptors.
Tetrahydronaphthalenic ligands were synthesized and evaluated as melatonin receptor ligands. Biological studies show that the aromaticity of the ring bearing the side chain is not essential for affinity and activity and that replacement of the methoxy group with the bioisostere ethyl which does not offer the possibility of H-bonding, leads to antagonist or forskoline potentiating properties.
Fourmaintraux
E
E
Institut de Chimie Pharmaceutique, Lille, France.
Depreux
P
P
Lesieur
D
D
Guardiola-Lemaître
B
B
Bennejean
C
C
Delagrange
P
P
Howell
H E
HE
D000818:Animals; D001667:Binding, Competitive; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D011869:Radioligand Assay; D011956:Receptors, Cell Surface / Q000819:agonists* / Q000037:antagonists & inhibitors*; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000037:antagonists & inhibitors*; D044094:Receptors, Melatonin; D012756:Sheep; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000494:pharmacology*
D011956:Receptors, Cell Surface; D018160:Receptors, Cytoplasmic and Nuclear; D044094:Receptors, Melatonin; D013764:Tetrahydronaphthalenes; D005576:Colforsin; D000242:Cyclic AMP