Agonist activity of a novel compound, 1-[3-(3,4-methylenedioxyphenoxy)propyl]-4-phenyl piperazine (BP-554), at central 5-HT1A receptors.

Abstract

We used an in vitro radioligand receptor binding assay with rat cerebral cortex, hippocampus and striatum membrane preparations to show that 1-[3-(3,4-methylenedioxyphenoxy)propyl]-4-phenyl piperazine (BP-554) had much higher affinity for 5-HT1A recognition sites than for 5-HT1-non-A, 5-HT2, benzodiazepine, dopamine D-2 and alpha 2-adrenergic recognition sites. The compound inhibited the activity of forskolin-stimulated adenylate cyclase in rat hippocampal membranes. Intraperitoneal injection of BP-554 to mice decreased the concentration of only 5-hydroxy-indoleacetic acid of the amines and their metabolites in the brain and decreased the accumulation of 5-hydroxytryptophan in the brain after decarboxylase inhibition by 3-hydroxybenzylhydrazine. Furthermore, the administration of BP-554 caused hypothermia and increased serum corticosterone levels in mice. The observed effects of BP-554 were similar to those of 8-hydroxy-2-(di-n-propylamino)tetralin. These results suggest that BP-554 acts as a selective 5-HT1A receptor agonist in vivo.

• Authors: T Matsuda, Y H Seong, H Aono, T Kanda, A Baba, K Saito, A Tobe, H Iwata
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 170 Issue 1-2 Pg. 75-82 (Oct 24 1989) ISSN: 0014-2999 [Print] Netherlands
• PMID: 2533078 (Publication Type: Journal Article)

Chemical References

• Amines
• Piperazines
• Receptors, Serotonin
• Tetrahydronaphthalenes
• Colforsin
• 8-Hydroxy-2-(di-n-propylamino)tetralin
• BP 554
• Adenylyl Cyclases
• Corticosterone

Topics

• 8-Hydroxy-2-(di-n-propylamino)tetralin
• Adenylyl Cyclases (metabolism)
• Amines (metabolism)
• Animals
• Body Temperature (drug effects)
• Brain Chemistry (drug effects)
• Chromatography, High Pressure Liquid
• Colforsin (pharmacology)
• Corticosterone (blood)
• Kinetics
• Male
• Mice
• Mice, Inbred Strains
• Piperazines (pharmacology)
• Radioligand Assay
• Rats
• Rats, Inbred Strains
• Receptors, Serotonin (drug effects)
• Tetrahydronaphthalenes (pharmacology)