1.
Bioorg Med Chem Lett
; 15(23): 5253-6, 2005 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16168646
RESUMO
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.
Assuntos
Antipsicóticos/química , Antipsicóticos/farmacologia , Benzamidas/química , Benzamidas/farmacologia , Receptores de Dopamina D4/antagonistas & inibidores , Antagonistas do Receptor 5-HT2 de Serotonina , Antipsicóticos/síntese química , Benzamidas/síntese química , Dopamina/química , Humanos , Ligantes
2.
Bioorg Med Chem Lett
; 14(19): 4847-50, 2004 Oct 04.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15341937
RESUMO
A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure-activity relationships studied. Potent ligands selective for human D(4) (hD(4)) over hD(2) and alpha(1) have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC(50) of 1500 nM.