Opiods Flashcards
opioid:
morphine-like effects
opiate:
morphine-like structure
endogenous opioid peptides:
ekephaline
endorphins
dynorphins
which cells produce endogenous opioids?
neuronal and non-neuronal
opioid precursor polypeptides:
Preproenkephalin
Preproopiomelanocortin
Preprodynorphin
met and leu-enkephalins are derived from what prepro and propeptide?r
preproenkephalin and proenkephalin
Beta endorphin is derived from what prepro and pro peptide?
Preproopiomelanocortin
proopiomelanocortin(POMC)
preprodynorphin is cleaved to produce what?
prodynorphin
Golgi retention sequences are found at which stage of opiod synthesis?
preprohormone
cleaving of preprohormone is undertaken by what enzymes?
endopeptidases
which opioid receptor promotes analgesia at the spinal level?
kappa
which receptor is the target of most analgesic opioids?
mu
where do delta receptors promote analgesia?
periphery
ORL endogenous ligand:
nociceptin
describe the selectivity of beta-endorphin.
high, equal affinity to all 3 receptors
which opioids do not exhibit affinity for the kappa receptor?
met and leu-enkephalin
how do the enkephalins differ in their affinity?
leu displays less affinity for mu
important site of opioid action:
GIT
CNS
respiratory system
analgesia components:
nociception and affective
which G protein are opioid receptors coupled to?
Galpha i/o
effect of opioid receptor activation on adenyl cyclase?
inhibit
reduce cAMP
DAMGO
opioid agonist
high mu specificity
which K+ channels do opioids activate?
Kir
Which channels do opioids inhibit?
voltage-gated calcium channels
which portion of GPCR binds to ion channels?
Beta Gamma dimer
the direction of afferent information:
DRG
superior dorsal horn
thalamus
somatosensory cortex
