1997, FEBS Lett 412, 35–38; Walker et al., 1999, Eur J Pharmacol 383,
115–119). A unique 6-MAM/M6G subreceptor or splice variant responsible
for their analgesic activity has been proposed. Whether this also accounts
for the stimulating properties of these opioids, has however not been
investigated. Therefore, we explored the antagonizing effects of 3-
MeONtx and naltrexone (NTX) on the acute stimulating effects of
heroin, 6-MAM and morphine in mice, and their pharmacokinetic profiles.
3-MeONtx (0.5 or 2.5 mg/kg) or NTX (0.05 or 0.5 mg/kg) was given intra-
peritoneally 15 min before heroin (5–50 mmol/kg), 6-MAM (5–50 mmol/kg)
or morphine (10–80 mol/kg) was administered subcutaneously in male
C57BL/6 J mice. The locomotor activity was then recorded for 1 h. Separate
groups of mice were sacrificed at different time points following antagonist
administration, and their brains were analyzed for 3-MeONtx or NTX using
LC-MS/MS. Pretreatment with 3-MeONtx blocked the increase in
locomotor activity induced by heroin, 6-MAM, and morphine. Administra-
tion of 3-MeONtx or NTX gave similar pharmacokinetic profiles in mouse
brain, and besides potency disparities, no clear difference in antagonizing
effect was observed between 3-MeONx and NTX. 3-MeONtx is no more
selective in antagonizing the acute stimulating effects of heroin and 6-
MAM than that of morphine in mice. This indicates that the stimulating
effects of these opioids are mediated by a population of similar m-OR, and
further that their analgesic- and stimulating effects are mediated by
different m-OR splice variants or mechanisms in mice.
E.14 - EFFECTS OF CURCUMIN ON BRAIN
STIMULATION REWARD AND THE REWARD-
FACILITATING EFFECT OF MORPHINE
Vicky Katsidoni
a
, Marilena Fotiadou
b
, Marina Sagnou
c
and
George Panagis
a
a
University of Crete, Department of Psychology, Laboratory of Behavioral
Neuroscience, 74100 Rethymno, Crete,
b
City Unity College, Department of
Psychology, 15-17Thiseos str, Syntagma,Athens, T.K. 10562 and
c
National Centre
for Scientific Research Demokritos, Institute of Biology, 15310 Ag. Paraskevi,
Attiki, Athens, Greece
Curcumin is a multimodal polyphenol natural product isolated from
the plant Curcuma longa. Recent animal studies reported that curcumin
has several central actions, among which are an antidepressant and a
neuroprotective effect. In the present study we utilized the intracranial
self-stimulation (ICSS) paradigm to examine the effects of the
commercially available curcuminoid mixtrure, pharmaceutically used as
food supplement, on brain reward and on the reward-facilitating effect
of morphine. To the best of our knowledge, this is the first study on the
effects of curcumin on brain stimulation reward and the reward-
facilitating effect of opioids. Male Sprague-Dawley rats were implanted
with a monopolar electrode into the medial forebrain bundle (MFB) and
were trained to respond for electrical stimulation using a rate-frequency
paradigm. In the first experiment, rats were injected with curcumin (5,
10 and 20 mg/kg, i.p.). The highest doses of curcumin tested
significantly increased the threshold frequency required for MFB ICSS.
In a second experiment, we examined whether curcumin (5 mg/kg, i.p.)
could counteract the reward-facilitating effect of morphine (10 mg/kg,
s.c.). Curcumin inhibited the reward-facilitating effect of morphine, at a
dose that did not by itself affect brain reward function. The present
results indicate that curcumin does not exhibit reinforcing properties in
the ICSS paradigm over a range of doses tested, but rather has an
inhibitory influence on reward mechanisms at high doses and even
reduces the reward-facilitating effect of morphine. The present data
indicate that curcumin interferes with brain reward mechanisms
responsible for the expression of the acute reinforcing properties of
opioids and provide evidence that curcumin may be used as a food
supplement in attenuating the rewarding effects of opioids.
E.15 - GHRELIN RECEPTOR ANTAGONISM
ATTENUATES MORPHINE-INDUCED ACCUMBAL
DOPAMINE RELEASE AND BEHAVIORAL
STIMULATION IN RATS
Sustkova-Fiserova Magdalena
a
, Jerabek Pavel
a
, Havlickova
Tereza
a
, Kacer Petr
b
and Krsiak Miloslav
a
a
Department of Pharmacology, 3rd Faculty of Medicine, Charles University,
Ruska 87, Prague 10, 100 34 and
b
Laboratory of medicinal diagnostics,
Department of organic technology ICT, Technicka 5, Prague 6, 166 28, Czech Republic
Aims of the study: An orexigenic appetite regulating peptide ghrelin
activates binding sites in the ventral tegmental area, a structure linked
with reward, thus probably participating in reward-seeking behavior. An
increasing number of studies during the last years indicates ghrelin ´s
participation in alcohol abuse, several also focused on cocaine and
nicotine abuse. However the role of ghrelin in opioid dependence has
been only rarely studied yet. Thus, we wanted to determine, whether
the central ghrelin signaling system participates also in the reward
processes of opiods, namely morphine.
Methods: We used ‘‘in vivo’’ microdialysis to determine the changes
in concentrations of dopamine and its metabolites in the nucleus
accumbens shell (NACSh) in rats following morphine (MO, 5, 10 mg/kg
s.c.) injection with or without ghrelin antagonist pretreatment (JMV2959,
6 mg/kg i.p. 20 min before MO). The induced behavioral changes were
simultaneously monitored.
Results: For both doses morphine-induced behavioral stimulation was
significantly reduced by the JMV2959 pretreatment, especially with
regards to stereotypes. JMV2959 also significantly reduced the
morphine-induced enhancement of accumbal dopamine release. The
morphine-induced enhanced dopamine metabolism was also influenced
by JMV2959 pretreatment (after pretreatment owith the lower MO
dose, accumbal 3-MT level was decreased, while DOPAC and HVA
levels were increased after pre-treatment with the higher MO dose).
Conclusion: GHS-R1A appears to be required for opioid-induced
reward. Our data confirm that the central ghrelin signaling system might
constitute a novel potential target for the treatment of drug
dependence. This work was supported by projects IGA MHCR NT/
13687–3/2012, GAUK 54313 and PRVOUK P34.
E.16 - SELECTIVE MODULATION OF THE MOTOR
SUPPRESSANT EFFECTS OF NICOTINE BY THE GABA-
A RECEPTOR ANTAGONIST, BICUCULLINE
Rajeev I. Desai
a
and Philip Terry
b
a
Preclinical Pharmacology Laboratory, McLean Hospital/Harvard Medical
School, Belmont, MA 02478, USA and
b
Department of Psychology, Kingston
University London, Kingston-upon-Thames, Surrey KT1 2EE, UK
The acute administration of nicotine reliably produces dose- and
time-dependent decreases in motor activity in laboratory rodents;
however, the neurochemical mechanisms that underlie this effect have
not yet been identified. The present series of experiments was
conducted to evaluate the contributions of nicotinic, dopaminergic,
and GABAergic receptor mechanisms in the acute motor suppressant
effects of nicotine. Using a time-sampling observational procedure, the
effects of nicotine alone and in combination with a nicotinic
(mecamylamine), dopaminergic (flupenthixol), GABA-A (bicuculline),
and GABA-B (saclofen) receptor antagonist were determined over a
40 min observation period in male CD1 mice (n = 8/treatment group).
Nicotine (0.1–1.0 mg/kg) alone produced a dose-related and time-
dependent decline in motor activity (i.e., immobility frequency
EBPS Workshop Abstracts e45
Copyright © Lippincott Williams & Wilkins. Unauthorized reproduction of this article is prohibited.