1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 receptors over cloned African Green monkey D2 receptors was observed with 1-(2-pyridyl)-4-[[3-(1-phenylpyrrolyl)]methyl]piperazine.
Thurkauf
A
A
Department of Chemistry, Neurogen Corporation, Branford, Connecticut 06405, USA.
Yuan
J
J
Chen
X
X
Wasley
J W
JW
Meade
R
R
Woodruff
K H
KH
Huston
K
K
Ross
P C
PC
D000818:Animals; D014150:Antipsychotic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D003001:Cloning, Molecular; D006801:Humans; D006860:Hydrogen Bonding; D009682:Magnetic Resonance Spectroscopy; D011758:Pyrroles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D011954:Receptors, Dopamine / Q000145:classification / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D011758:Pyrroles; D011954:Receptors, Dopamine; D011994:Recombinant Proteins