Characterization of N,N(Me)2-Dmt-Tic-OH, a delta selective opioid dipeptide antagonist

Autor(en)

K Monory, S D Bryant, I Kertész, G Balboni, R Guerrini, G Tóth, S Salvadori, L H Lazarus, A Borsodi

Abstrakt

N,N(Me)2-Dimethyl-tyrosine-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-OH (N,N(Me)2-Dmt-Tic-OH) is a very selective delta opioid dipeptide with elevated antagonist activity. We have radiolabelled this compound by catalytic tritiation of the N,N(Me)2-Dmt(3',5'-I2)-Tic-OH precursor. The ligand labelled rat brain membranes with a Kd value of 0.42 nM and a Bmax of 63.12 fmol/mg protein. The new tritiated ligand showed high affinity for the delta opioid receptor whereas its binding at mu and kappa opioid receptors was weak. N,N(Me)2-Dmt-Tic-OH was able to inhibit the agonist-stimulated binding of the non-hydrolysable GTP analogue ¿35SGTPgammaS, thus attenuating the activation of G proteins via opioid receptors. This simple opioid dipeptide in both normal and labelled form may serve as a useful tool to study delta opioid receptors in vitro and in vivo.

Organisation(en)

Department für Pharmazeutische Wissenschaften, Institut für Praktische Theologie

Externe Organisation(en)

Hungarian Academy of Sciences, National Institute of Environmental Health Sciences

Journal

NEUROREPORT

Band

11

Seiten

2083-6

Anzahl der Seiten

4

ISSN

0959-4965

DOI

https://doi.org/10.1097/00001756-200007140-00005

Publikationsdatum

07-2000

Peer-reviewed

Ja

ÖFOS 2012

301207 Pharmazeutische Chemie

Schlagwörter

Link zum Portal

https://ucrisportal.univie.ac.at/de/publications/characterization-of-nnme2dmtticoh-a-delta-selective-opioid-dipeptide-antagonist(442e7b0f-24e2-4013-bd97-a86b19db5759).html