1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors.
We report the synthesis of and binding to the two subtypes of mouse thyrotropin-releasing hormone (TRH) receptors, TRH-R1 and TRH-R2, of several 1-(phenyl)isoquinoline carboxamide analogues. These analogues showed a degree of selectivity for binding at TRH-R2. These are the first ligands reported that show selective binding to these receptors.
Jiang
Jian-Kang
JK
Chemical Biology Core Facility, National Institute of Diabetes and Digestive and Kidney Disorders, National Institutes of Health, Bethesda, MD 20892-1818, USA.
Thomas
Craig J
CJ
Neumann
Susanne
S
Lu
Xinping
X
Rice
Kenner C
KC
Gershengorn
Marvin C
MC
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D007546:Isoquinolines / Q000138:chemical synthesis / Q000494:pharmacology*; D008024:Ligands; D051379:Mice; D011869:Radioligand Assay; D018025:Receptors, Thyrotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000577:Amides; D007546:Isoquinolines; D008024:Ligands; D018025:Receptors, Thyrotropin-Releasing Hormone