The action of a synthetic derivative of Met5-enkephalin-Arg6-Phe7 on behavioral and endocrine responses.

Abstract:

:The neuroendocrine and behavioral effects of Tyr-D-Ala-Gly-Phe-D-Nle-Arg-Phe (DADN), a more stable derivative of the endogenous opiate Met-enkephalin related peptide Met(5)-enkephalin-Arg(6)-Phe(7) were investigated in mice. The behavioral experiments consisted of monitoring the horizontal (square crossing) and vertical (rearing) locomotion in the open field system. To evaluate the effect of the heptapeptide on the hypothalamo-pituitary-adrenal (HPA) axis, the plasma corticosterone level was measured. DADN induced dose-dependent increases in locomotion and rearing 30 min after intracerebroventricular injection and also elicited marked activation of the hormonal stress response. To elucidate the receptors involved in the mediation of these actions, animals were pretreated with the nonselective opioid antagonist naloxone, the selective κ-receptor antagonist nor-binaltorphimine or the μ(1)-receptor blocker naloxonazine. Both the HPA activation and the behavioral responses were diminished by the preadministration of naloxone. Nor-binaltorphimine did not display a significant effect, while naloxonazine completely abolished the hyperactivity and the corticosterone elevation elicited by the analog. These findings suggest that μ-receptors predominate in the mediation of the neuroendocrine actions of DADN, while κ-receptors do not play a significant role.

journal_name

Peptides

journal_title

Peptides

authors

Csabafi K,Jászberényi M,Bagosi Z,Tóth G,Wollemann M,Telegdy G

doi

10.1016/j.peptides.2011.05.029

subject

Has Abstract

pub_date

2011-08-01 00:00:00

pages

1656-60

issue

8

eissn

0196-9781

issn

1873-5169

pii

S0196-9781(11)00238-5

journal_volume

32

pub_type

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