摘要
The term “opioid” generally refers to any substance,
endogenous or synthetic peptide or non-peptide, which acts through any of the
four major types of opioid receptors present in the cell membrane. Its
effects can be stereospecifically blocked by pure narcotic antagonists like
naloxone. The four major classes of endogenous opioid peptides, b-endorphin, enkephalin, dynorphin and
nociceptin have been described as potential ligands for the m, d,
k and opioid receptor like (ORL1)
receptor binding sites. Opioid peptides and their receptors are implicated in
the modulation of a number of behavioral and physiological functions in birds
(e.g., reproduction, endocrinology, water balance, social behavior and
painful stimulus) in a manner similar to that described for mammals. Opioids are (neuro) peptides, which are synthesized in the central nervous
system (CNS) in the whole animal kingdom. They play a role both as
neurotransmitters and neuromodulators.Opioid peptides and their
receptors are implicated in the modulation of a number of behavioral and
physiological functions in birds (e.g., reproduction, endocrinology, water
balance, social behavior and painful stimulus) in a manner similar to that
described for mammals. Nowadays, more attention is being paid to the effect
of the opioid system on the water balance in birds. Opioid drugs were also
introduced in veterinary medicine for pain relieving and anesthesia of birds.
The studies reported in
this dissertation were undertaken to further elucidate opioid receptors, the
physiological intervention on receptor binding properties and their
regulation. To this end, we evaluated the receptor binding profiles - the
dissociation constant (Kd) and maximum binding capacity (Bmax) - in various
brain regions. Following questions were addressed using the chicken as model.
Are opioid binding
profiles gender-, and/or age-dependent in the chicken brain?
Are opioid binding profiles affected by dehydration in the chicken brain?
Are opioid binding profiles testosterone-dependent?, and
Are opioid binding profiles affected by opioid antagonist?
To achieve this, the
opioid binding sites were determined in six brain regions - frontal cortex,
lateral septum, striatum, amygdala, hippocampus and hypothalamus - of chicken
using [3H]diprenorphine ([3H]DPN) as the radioligand. Three
age groups of chickens, 10-day-, 10-week- and 26-38-week-old, were used. Following
situations were considered (a) the effects of hydration (b) the effect of
testosterone treatments (performed in castrated male chickens) and (c) the
effect of opioid antagonist, naltrexone.
Experiment I, opioid binding sites were
investigated in 10-day-, 10-week- and 26-38-week-old female and male
chickens. The linear Scatchard plot of [3H]DPN binding in all
experiments indicated a single binding site with high affinity. The mean of
Bmax was as following: 0.27-0.44 (female), 0.23-0.33 (male); 0.21-0.48
(female), 0.21-0.41 (male); 0.19-0.34 (female), 0.17-0.34 (male) pmol/mg in
10-day-, 10-week- and 26-38-week-old chickens, respectively. The mean of Kd
was as follow: 1.13-1.80 (female), 0.72-1.01 (male); 0.28-0.48
(female), 0.27-0.83 (male); 0.33-0.75 (female), 0.26-0.58 (male) nM in
10-day-, 10-week- and 26-38-week-old chickens, respectively. The
highest concentration of opioid binding sites was found in the frontal cortex
and the lowest concentration in the hypothalamus both in males and females. The
Bmax of opioid binding sites decreased significantly from 10-day-old to
adulthood in the frontal cortex, striatum and amygdala regions. While there
was no such a decrease in males. The data also indicated that the sex related
change in opioid binding reflects a change in the Kd in males more than in
females.
Experiment II, groups of 10-day-, 10-week- and
26-38-week-old chickens were deprived from water for 1 or 2 days. Dehydration
induced an increase of plasma AVT levels and had some impacts on the
characteristics of opioid binding sites in the brain. Most of the
changes of opioid binding site were in young female chickens. The results also
indicated that dehydration induced both decrease (frontal cortex, striatum
and amygdala: 10-day-old females; lateral septum: adult females; and
hypothalamus: 10-day-old males) and increase (lateral septum, hippocampus and
hypothalamus: 10-week-old females) of Bmax in chicken brains. Such changes
were accompanied with alterations in receptor affinity.
Experiment III, male chickens were castrated and
sham-operated for 7 months and were treated with testosterone proprionate or
testosterone proprionate and naltrexone. The Bmax value in the brain of
castrated chickens was higher than that found in intact animals. This
increase was testosterone-dependent, since testosterone substitution reduced
the binding capacity to the control levels. The
extent of opioid binding site changes after naltrexone administration was more pronounced in the Kd than in the Bmax values. The
regional differences in naltrexone-induce changes imply that the drug does
not have uniform effects throughout the brain. The Bmax was significantly
increased in the hypothalamus only.
In
conclusion, these results demonstrate, that like in some mammals, opioid
binding sites are involved in modulation of water balance and reproduction in
chickens. Such modulations
are age-, sex- and brain region dependent.