Effect of GNTI, a kappa opioid receptor antagonist, on MK-801-induced hyperlocomotion and stereotypy in mice.
by
Qi CT, Zou H, Zhang CH, Xie QL, Jin ML, Yu L.
Research Center for Biotechnology,
Shanghai Institutes for Biological Sciences,
Chinese Academy of Sciences,
Shanghai 200233, China.
Acta Pharmacol Sin. 2006 Nov;27(11):1401-8.


ABSTRACT

AIM: To examine the effect of GNTI [5'-guanidinyl-17-(cyclopropylmethyl)-6,7- dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan], a selective antagonist for the kappa opioid receptor, in the MK-801 (dizocilpine maleate)-induced behavioral model of psychosis in schizophrenia as a way to explore the involvement of the kappa opioid receptor in modulating psychotic symptoms of schizophrenia. METHODS: Two doses of MK-801 (0.3 mg/kg and 0.6 mg/kg) were administered by systemic injection in mice to induce psychosis-like behavior as a rodent schizophrenia model, preceded by an injection of different doses of GNTI. Both locomotion and stereotypy were measured as the behavioral endpoints for quantitative analysis. RESULTS: GNTI inhibited MK-801-induced hyperlocomotion and stereotypy. In particular, GNTI showed differential modulation of stereotypy induced by 0.3 mg/kg vs 0.6 mg/kg MK-801. CONCLUSION: Antagonism of kappa opioid receptors attenuates MK-801-induced behavior, suggesting a potential involvement of the kappa opioid receptor in psychosis-like symptoms of schizophrenia. GNTI appears to be a useful pharmacological tool to explore the kappa opioid receptor function in vivo.
JDTic
Nor-binaltorphimine
Fentanyl and ketamine
Kappa upregulation and addiction
kappa-Opioid withdrawal in planaria
The mesolimbic kappa-opioid system
Kappa opioid agonists make rats depressed
Kappa antagonists as future antidepressants?
Nalbuphine and anti-analgesia in men and women
Stress, dysphoria and the dynorphin kappa-opioid system
Indolomorphinan antagonists of the kappa-opioid receptor
The kappa receptor antagonist norbinaltorphimine as an antidepressant
JDTic: an antidepressant, anxiolytic kappa-selective opioid receptor antagonist


Refs
and further reading

HOME
HedWeb
Nootropics
erythroxylum-coca.com
Future Opioids
BLTC Research
MDMA/Ecstasy
Superhapiness?
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Good Drug Guide

The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family