Aminotriazine 5-HT7 antagonists

Ronald J Mattson; Derek J Denhart; John D Catt; Michael F Dee; Jeffrey A Deskus; Jonathan L Ditta; James Epperson; H Dalton King; Aiming Gao; Michael A Poss; Ashok Purandare; David Tortolani; Yufen Zhao; Hua Yang; Suresh Yeola; Jane Palmer; John Torrente; Arlene Stark; Graham Johnson

doi:10.1016/j.bmcl.2004.06.008

Aminotriazine 5-HT7 antagonists

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4245-8. doi: 10.1016/j.bmcl.2004.06.008.

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-7660, USA. [email protected]

PMID: 15261279
DOI: 10.1016/j.bmcl.2004.06.008

Abstract

The present studies have identified a series of aminotriazines as novel 5-HT(7) receptor antagonists. Compounds 10 and 17 have high affinity for the 5-HT(7) receptor and do not bind to either the 5-HT(2C) or 5-HT(6) receptors. These compounds produce no agonist effects by themselves, and shift the dose-response curve of 5-CT to the right in the manner of an antagonist.

MeSH terms

Dose-Response Relationship, Drug
Receptors, Serotonin / drug effects*
Serotonin Antagonists / pharmacology*
Triazines / pharmacology*

Substances

Receptors, Serotonin
Serotonin Antagonists
Triazines
serotonin 7 receptor