Abstract
The optimisation of affinity and selectivity in a novel series of dual 5-HT5A/5-HT7 receptor ligands is described. Brain penetrant 2-aminodihydroquinazolines with low nanomolar affinities were identified.
MeSH terms
-
Brain / metabolism
-
Guanidines / chemistry
-
Guanidines / metabolism*
-
Guanidines / pharmacokinetics
-
Guanidines / pharmacology
-
Humans
-
Kinetics
-
Ligands
-
Pyrimidines / chemistry
-
Pyrimidines / metabolism
-
Pyrimidines / pharmacokinetics
-
Pyrimidines / pharmacology
-
Quinazolines / chemistry
-
Quinazolines / metabolism*
-
Quinazolines / pharmacokinetics
-
Quinazolines / pharmacology
-
Receptors, Serotonin / chemistry
-
Receptors, Serotonin / metabolism*
-
Structure-Activity Relationship
Substances
-
Guanidines
-
Ligands
-
Pyrimidines
-
Quinazolines
-
Receptors, Serotonin
-
serotonin 5 receptor
-
serotonin 7 receptor