Synthesis and radioreceptor binding activity of N-0437, a new, extremely potent and selective D2 dopamine receptor agonist.
The synthesis of a new, potent and selective D2 dopamine receptor agonist, N-0437, of the 2-aminotetralin group is described. The results of a radioreceptor binding assay using a homogenate of porcine anterior pituitary as a tissue source for D2 dopamine receptors and 3H-spiperone as radioligand demonstrate that this compound is one of the most potent compounds so far evaluated in this test system.
Horn
A S
AS
Tepper
P
P
Van der Weide
J
J
Watanabe
M
M
Grigoriadis
D
D
Seeman
P
P
D000818:Animals; D001667:Binding, Competitive; D066298:In Vitro Techniques; D009281:Naphthalenes / Q000138:chemical synthesis*; D011869:Radioligand Assay; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000378:metabolism; D013329:Structure-Activity Relationship; D013552:Swine; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology; D014316:Tritium
D009281:Naphthalenes; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; D014316:Tritium; D013134:Spiperone; C047508:rotigotine