Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors

Four 7-[3-(4-phenyl-1-piperazinyl)propoxy]coumarins were synthesized. The affinities of these compounds for DA (D2A, D3) and 5HT1A receptors were evaluated for their ability to displace [3H]-raclopride and [3H]-8-OH-DPAT respectively from their specific binding sites. The affinities of the target co...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-12, Vol.8 (24), p.3567-3570
Hauptverfasser:	TERAN, C, SANTANA, L, URIARTE, E, FALL, Y, UNELIUS, L, TOLF, B.-R
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences CHO Cells Cricetinae Humans Medical sciences Mice Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperazines - chemistry Piperazines - metabolism Piperazines - pharmacology Radioligand Assay Receptors, Dopamine D2 - drug effects Receptors, Dopamine D2 - metabolism Receptors, Dopamine D3 Receptors, Serotonin - drug effects Receptors, Serotonin - metabolism Receptors, Serotonin, 5-HT1 Serotoninergic system
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Zusammenfassung:	Four 7-[3-(4-phenyl-1-piperazinyl)propoxy]coumarins were synthesized. The affinities of these compounds for DA (D2A, D3) and 5HT1A receptors were evaluated for their ability to displace [3H]-raclopride and [3H]-8-OH-DPAT respectively from their specific binding sites. The affinities of the target compounds were all in the nanomolar range and followed the order 5-HT1A > D2 > D3.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00646-5