Aminotriazine 5-HT7 antagonists.
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.
Mattson
Ronald J
RJ
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-7660, USA. mattsonr@bms.com
Denhart
Derek J
DJ
Catt
John D
JD
Dee
Michael F
MF
Deskus
Jeffrey A
JA
Ditta
Jonathan L
JL
Epperson
James
J
Dalton King
H
H
Gao
Aiming
A
Poss
Michael A
MA
Purandare
Ashok
A
Tortolani
David
D
Zhao
Yufen
Y
Yang
Hua
H
Yeola
Suresh
S
Palmer
Jane
J
Torrente
John
J
Stark
Arlene
A
Johnson
Graham
G
D004305:Dose-Response Relationship, Drug; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000494:pharmacology*; D014227:Triazines / Q000494:pharmacology*
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014227:Triazines; C104425:serotonin 7 receptor