The cardiovascular effects of PFRFamide and PFR(Tic)amide, a possible agonist and antagonist of neuropeptide FF (NPFF).
Neuropeptide FF (NPFF), an endogenous opioid-related neuromodulater, has been reported to show significant effects on the cardiovascular system, namely elevation of arterial blood pressure (BP) and heart rate (HR) in rats. In the present study, we synthesized two novel NPFF analogs, PFRFamide (putative NPFF agonist) and PFR(Tic)amide (putative NPFF antagonist), and examined their cardiovascular effect on BP and HR in anesthetized rats. The arterial mean BP and HR were measured by way of direct femoral artery catheterization. The data showed that PFRFamide increased BP in a dose-dependent manner, while PFR(Tic)amide decreased BP dose-dependently. These results revealed the possibility of PFRFamide and PFR(Tic)amide to be NPFF agonist and antagonist (or inverse agonist), respectively. These two NPFF analogs may possess potential in new drug design, and the NPFF system could be very important in mammalian cardiovascular function.
Huang
E Y
EY
Department and Institute of Pharmacology, National Yang-Ming University, Taipei, Taiwan.
Li
J Y
JY
Tan
P P
PP
Wong
C H
CH
Chen
J C
JC
D000577:Amides / Q000138:chemical synthesis; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002319:Cardiovascular System / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D009479:Neuropeptides / Q000494:pharmacology*; D009842:Oligopeptides / Q000819:agonists* / Q000037:antagonists & inhibitors*; D010455:Peptides / Q000138:chemical synthesis; D051381:Rats; D017207:Rats, Sprague-Dawley; D044005:Tetrahydroisoquinolines
D000577:Amides; D009479:Neuropeptides; D009842:Oligopeptides; C402062:PFR(Tic)amide; D010455:Peptides; D044005:Tetrahydroisoquinolines; C402043:prolyl-phenylalanyl-arginyl-phenylalaninamide; C053651:phenylalanyl-leucyl-phenylalanyl-glutaminyl-prolyl-glutaminyl-arginyl-phenylalaninamide