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Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr: a new highly potent and fully specific agonist for opiate delta-receptors.

Abstract：

:Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr (DTLET) was rationally designed as pure delta-probe from proposed models of mu and delta opiate receptors. On peripheral organs, deltakephalin displays a 3000 times higher inhibitory potency on the electrically stimulated mouse vas deferens (IC50 = 0.15 nM) as on the guinea pig ileum (IC50 = 460 nM). As expected [3H]deltakephalin interacts at 35 degrees C in rat brain tissue to a single class of binding sites (delta) (Bmax = 0.115 pmole/mg protein) with a high affinity: KD = 1.35 nM from equilibrium measurements and KD = 0.43 nM from kinetic determinations. Deltakephalin occurs as the most specific ligand for delta-binding sites as shown by the following discrimination ratios KI(mu)/KI(delta): 0.31 for D-Ala2-D-Leu5-enkephalin; 0.15 for D-Ser2-Thr6-Leu-enkephalin and 0.05 for deltakephalin.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Zajac JM,Gacel G,Petit F,Dodey P,Rossignol P,Roques BP

doi

10.1016/0006-291x(83)90318-2

subject

Has Abstract

pub_date

1983-03-16 00:00:00

pages

390-7

issue

2

eissn

0006-291X

issn

1090-2104

pii

0006-291X(83)90318-2

journal_volume

111

pub_type

杂志文章

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