Serotomide and safflomide modulate forskolin-stimulated cAMP formation via 5-HT1 receptor.
Serotomide (trans-N-caffeoylserotonin) and safflomide (trans-N-caffeoyltryptamine) belong to serotonin-derived phenylpropenoid amides found in plants. In this paper, serotomide and safflomide were investigated to determine their effects on serotonin receptor 5-HT1 in the renal epithelial (OK) cells, due to their structural similarity to 5-HT1 receptor ligands. At the concentration of 10 microM, serotomide was able to inhibit forskolin-stimulated cAMP formation in the OK cells by 31% (p<0.019). The inhibition was repressed by Nan-190 and spiperone (5-HT1 antagonists), suggesting that serotomide suppresses cAMP formation via binding to 5-HT1 receptors in the OK cells. Meanwhile, safflomide could not inhibit forskolin-stimulated cAMP formation at the same concentration (10 microM), but repress the inhibition of forskolin-stimulated cAMP by serotonin agonists (e.g., serotonin and 8-OH-DPAT) by 31% (p<0.018), suggesting that safflomide may block 5-HT1 receptors in a similar way to Nan-190 and spiperone. All together the data indicate that serotomide and safflomide may be potent compounds that respectively act to activate and to block 5-HT1 receptors on OK cells.
Park
J B
JB
Diet, Genomics, and Immunology Laboratory, BHNRC, ARS, USDA, Beltsville, MD 20705, USA. jae.park@ars.usda.gov
D000818:Animals; D002109:Caffeic Acids / Q000494:pharmacology*; D002460:Cell Line; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000096:biosynthesis*; D009893:Opossums; D012701:Serotonin / Q000031:analogs & derivatives* / Q000494:pharmacology; D058825:Serotonin 5-HT1 Receptor Agonists; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists / Q000494:pharmacology; D014363:Tryptamines / Q000494:pharmacology*
D002109:Caffeic Acids; C534691:N-caffeoylserotonin; C521542:N-caffeoyltryptamine; D058825:Serotonin 5-HT1 Receptor Agonists; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists; D014363:Tryptamines; D005576:Colforsin; D012701:Serotonin; D000242:Cyclic AMP