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