Abstract
Novel, flexible arylpiperazine gepirone analogs (1a-3a) with a mixed 5-HT1A/5-HT2A receptor profile, low D2 receptor affinity, and agonistic (2a) or partial agonistic (1a, 3a) activity toward 5-HT1A receptor sites were synthesized. Their conformationally restricted counterparts (1b-3b) were selective 5-HT1A ligands (over 5-HT2A and D2 receptors), which turned out to be agonists (2b, 3b), or partial agonist (1b) of 5-HT1A receptors.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Dopamine Agonists / chemical synthesis
-
Dopamine Agonists / chemistry
-
Dopamine Agonists / pharmacology
-
Magnetic Resonance Spectroscopy
-
Male
-
Mice
-
Pyrimidines / chemical synthesis*
-
Pyrimidines / chemistry
-
Pyrimidines / pharmacology*
-
Rats
-
Rats, Wistar
-
Receptor, Serotonin, 5-HT1A / drug effects*
-
Receptor, Serotonin, 5-HT2A / drug effects*
-
Receptors, Dopamine D2 / drug effects*
-
Serotonin Receptor Agonists / chemical synthesis
-
Serotonin Receptor Agonists / chemistry
-
Serotonin Receptor Agonists / pharmacology
Substances
-
Dopamine Agonists
-
Pyrimidines
-
Receptor, Serotonin, 5-HT2A
-
Receptors, Dopamine D2
-
Serotonin Receptor Agonists
-
Receptor, Serotonin, 5-HT1A
-
gepirone