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59 Cards in this Set

  • Front
  • Back
reduce all sensations (mostly known for pain) and a sense of well-being and euphoria
narcotic analgesics
opium contains
morphine, codeine, thebaine, narcotine
when inducing opiates, vomiting is a common side effect due to the morphine's effect on the
area postrema
if one drug is more effective than another at inducing a physiological effect, then
it should bind to the tissue at a lower concentration than does the less-effective drug
three major opioid receptor subtypes
u-receptor, s-receptor, k-receptor
this receptor has a high affinity for morphine and related opiates and is widely distributed in the brain and spinal cord
u-receptor
for u-receptors this occurs in the medial thalamus, periaqueductal gray, median raphe, and spinal cord
analgesia
for the u-receptor, reinforcement occurs in the
nucleus accumbens
for the u-receptor, cardiovascular and respiratory depression, cough control, inducing nausea, and vomiting occurs in the
brain stem
for the u-receptor, the role in sensory-motor integration occurs in the ____ and the ____
thalamus, striatum
this receptor has a distribution similar to, but more restricted than the u-receptor
s-receptor
for the s-receptor, this occurs in the neocortex, striatum, olfactory areas, substantia nigra, and the nucleus accumbens (4)
roles of olfaction, motor integration, reinforcement, and cognitive function
this receptor is identified by high-binding to ketocyclazocine, an opiate analog that produces hallucinations and dysphoria; has diff distribution than u and s receptors
k-receptor
k-receptors occur in these 4 areas
striatum, amygdala, hypothalamus, and pituitary
k-receptors may function in (3)
pain perception, feeding, temperature control
stimulation of this particular brain area causes ____ and the opiate antagonist ____ inhibits this effect
periaqueductal gray, causes analgesia, naloxone
one class of endogenous morphine receptor ligands and all are produced by processing of large propeptides
enkephalins
the three genes/propeptides
1) prodynorphin 2) proenkephalin 3) pro-opiomelanocortin
this gene/propeptide produces neoendorphin and dynorphins
prodynorphin
this gene/propeptide produces enkephalins
proenkephalin
this gene/propeptide produces enorphin and a number of non-opioid transmitters, including adrenogorticotropic hormone (stress hormone)
pro-opiomelanocortin
another class of endogenous morphine receptor ligands are the
endomorphins
this class of endogenous morphine receptor ligands bind selectively to this receptor and is as potent as morphine in pain relief
endomorphins, u-receptor
propeptides are located in these three areas
brain, spinal chord, peripheral nervous system
propeptides are concentrated in areas concerning ____ and ____
pain modulation, mood
pro-opiomelanocortin is in particularly high concentration in the
pituitary
this hormone increases pro-opiomelanocortin mRNA production, and thus a later increase in ____ from the pituitary
adrenocorticotropic, endorphins
with respect to the CNS, although some opioid neurons are _____ neurons, many are ________
projection, local interneurons
opioids do not themselves change the _______ activity, but change the way the _______ respond to other inputs
postsynaptic neuron x2
the _____ (derived from proenkephalin) are likely the natural ligand for the _____
enkephalins, s-receptor
the _____ (derived from prodynorphin) are likely the natural ligand for the ______
dynorphins, k-receptor
the _____ are likely the natural ligand for the u-receptor
endomorphins
the _____ (derived form pro-opiomelanocortin) are likely the natural ligand for both the __ and __ receptors
endorphins, u/s
opioid receptor-mediated cellular changes are
inhibitory
opioid receptors are ____ linked and therefore can change postsynaptic activity either by ____ or _____
G-protein; directly changing channel opening; alter second messenger production
opioid receptors can open _ channels, and thus causes _______
K, postsynaptic neuron hyperpolarization
opioid receptors can close __ channels on presynaptic terminals, and thus ____ transmitter release from one neuron to the other
Ca, reduce
for opioid neurons that are co-localized with other transmitters, ______ cause ______ of all the neuron's transmitters
opioid autoreceptors, reduced release
all three receptors also reduce _____ production
cAMP
early pain is carried rapidly conducting _______ to the _____ and ___ ________
myelinated fibers; primary and secondary somatosensory cortex
late pain is carried by slowly conducting _______ to ____ brain areas
non-myelinated fibers; limbic brain area
three general mechanisms of opioids inhibiting pain transmission
1) within spinal cord by small inhibitory interneurons 2) two descending pathways originating in the periaqueductal grey 3) at higher brain sites, emotional and hormonal aspects of pain response
in spinal pathways, primary sensory pain afferents can either ____ onto _____ carrying pain info to the brain, or via an ____ ____ ____
directly synapse, projection neurons; intervening excitatory interneuron
spinal pathways can be inhibited by descending inputs that either inhibit the _____ or the ____
projection neuron, interposed excitatory interneuron
periaqueductal grey neurons are rich in ____ and stimulation of this region induces _____
opioids, analgesia
periaqueductal grey neurons project to ____ cells in the _____
serotonergic cells; raphe nuclei
periaqueductal grey neurons also innervate _____ neurons in the ______
noradrenergic neurons, locus coeruleus
opiates reduce the threshold for ______ to be reinforcing
intracranial electrical stimulation
_____ also induce self-administration, and are believed to work through _ or _ receptors. _ receptor agonists are not self-administered
endorphins, u or s; k receptors
self-administration of opiates occurs when _____ containing the opiates is situated near the ____ _____ _____
microcannula; ventral tegmental neurons
opiates increase ______ neuron firing, thus it releases dopamine into the _____ _____
ventral tegmental; nucleus accumbens
_ receptor agonists decrease _____ neuron firing
ventral tegmental
endorphins and other reinforcing opiates inhibit _____ neurons in the VTA, which _____ inhibition to the dopaminergic neurons, increasing their firing
GABAergic; decreases
____ and similar k receptor agonists presynaptically ____ dopamine release in the nucleus accumbens
dynorphin; inhibit
3 mechanisms of tolerance
1) increased rate of metabolism 2) classical conditioning 3) due to changes in nerve cells that compensate for chronic presence of opioids
two areas of brain that play major role in withdrawal syndrome
periaqueductal grey and locus coeruleus
despite its importance in reinforcement, injecting opiate antagonists in the ____ does not induce physical withdrawal symptoms
nucleus accumbens
acute morphine administration inhibits ____, which produces ____
adenylyl cyclase, cAMP
co-administration of _____ with _____ would block both cellular changes and conditioning, and thus reduces development of dependence
NMDA receptor antagonists; opiates