1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors

Jian-Kang Jiang; Craig J Thomas; Susanne Neumann; Xinping Lu; Kenner C Rice; Marvin C Gershengorn

doi:10.1016/j.bmcl.2004.11.017

1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors

Bioorg Med Chem Lett. 2005 Feb 1;15(3):733-6. doi: 10.1016/j.bmcl.2004.11.017.

Authors

Jian-Kang Jiang¹, Craig J Thomas, Susanne Neumann, Xinping Lu, Kenner C Rice, Marvin C Gershengorn

Affiliation

¹ Chemical Biology Core Facility, National Institute of Diabetes and Digestive and Kidney Disorders, National Institutes of Health, Bethesda, MD 20892-1818, USA.

PMID: 15664847
DOI: 10.1016/j.bmcl.2004.11.017

Abstract

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.

MeSH terms

Amides / chemical synthesis*
Amides / pharmacology
Animals
Binding, Competitive
Isoquinolines / chemical synthesis
Isoquinolines / pharmacology*
Ligands
Mice
Radioligand Assay
Receptors, Thyrotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Amides
Isoquinolines
Ligands
Receptors, Thyrotropin-Releasing Hormone

Grants and funding

Z01 DK070005-04/Intramural NIH HHS/United States