The neuropeptide FF analogue, 1DMe, acts as a functional opioid autoreceptor antagonist in the rat spinal cord.
We assessed the possible influence of a neuropeptide FF analogue, 1DMe ([D-Tyr(1),(NMe)Phe(3)]neuropeptide FF), on the inhibitory action of endogenous and exogenous partial differential-opioid receptor agonists on K(+)-evoked [Met(5)]-enkephalin release from superfused rat spinal cord slices. 1DMe (0.1-10 microM) dose-dependently enhanced the increase in superfusate [Met(5)]-enkephalin content due to the peptidase inhibitors thiorphan (1 microM) and bestatin (20 microM), and prevented the reduction in [Met(5)]-enkephalin release due to stimulation of partial differential receptors by 1 microM deltorphin I. Because it had the same effects as partial differential-opioid receptor antagonists, 1DMe might act through the functional blockade of presynaptically located partial differential-opioid autoreceptors.
Mauborgne
A
A
NeuroPsychoPharmacologie Moléculaire, Cellulaire et Fonctionnelle, INSERM U288, Faculté de Médecine Pitié-Salpêtrière, 91, Boulevard de l'Hôpital, 75634 cedex 13, Paris, France.
Bourgoin
S
S
Poliénor
H
H
Roumy
M
M
Simonnet
G
G
Zajac
J M
JM
Cesselin
F
F
D000818:Animals; D017660:Autoreceptors / Q000037:antagonists & inhibitors; D004305:Dose-Response Relationship, Drug; D004744:Enkephalin, Methionine / Q000378:metabolism; D066298:In Vitro Techniques; D007930:Leucine / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology*; D011188:Potassium / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013116:Spinal Cord / Q000187:drug effects* / Q000378:metabolism; D015244:Thiorphan / Q000494:pharmacology
D017660:Autoreceptors; D009292:Narcotic Antagonists; D009842:Oligopeptides; C105455:neuropeptide FF, Tyr(1)-N-methyl-Phe(3)-; C059567:deltorphin; D004744:Enkephalin, Methionine; D009271:Naltrexone; D015244:Thiorphan; C055382:naltrindole; D007930:Leucine; C012211:ubenimex; D011188:Potassium