N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor.
A series of N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides 8 has been prepared and found to bind with high affinity to the human D(4) (hD(4)) and 5-HT(2A) receptors. Several compounds displayed selectivity for these receptors versus hD(2) and alpha(1) adrenergic receptors of over 500-fold.
Arora
Jalaj
J
NPS Pharmaceuticals, 6850 Goreway Dr., Mississauga, Ont., Canada L4V 1V7.
Bordeleau
Michel
M
Dube
Laurence
L
Jarvie
Keith
K
Mazzocco
Lucy
L
Peragine
Jack
J
Tehim
Ashok
A
Egle
Ian
I
D014150:Antipsychotic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004298:Dopamine / Q000737:chemistry; D006801:Humans; D008024:Ligands; D050638:Receptors, Dopamine D4 / Q000037:antagonists & inhibitors*; D058830:Serotonin 5-HT2 Receptor Antagonists
D014150:Antipsychotic Agents; D001549:Benzamides; D008024:Ligands; D058830:Serotonin 5-HT2 Receptor Antagonists; D050638:Receptors, Dopamine D4; D004298:Dopamine