5.3 endogenous opioids and receptors Flashcards
preproopiomelancortin synthesized to
ACTH B-endorphin met-enkephalin leu-enkephalin Dynorphins A&B
ACTH
B-endorphin
anterior pituitary/immune
Preproenkephalin synthesized to
ACTH B-endorphin met-enkephalin leu-enkephalin Dynorphins A&B
met-enkephalin
leu-enkephalin
ens cns
preprodynorphin synthesized to
where
ACTH B-endorphin met-enkephalin leu-enkephalin Dynorphins A&B
Dynorphins A&B
leu-enkephalin
ENS CNS
mu, delta, and kappa receptors all cause
analgesia
- spinal
- supraspinal
Mu receptor causes
4
respiratory depression
inhibit GI motility
euphoria
miosis
K receptors
4
inhibit GI motility
psychotomimetic-(psychosis, delusions ,delirium, psychotic alteration of behavior and personality)
dysphoria
miosis
B-endorphin
receptor
main physiologic effect
mu delta
analgesia
met-enkephalin
leu-enkephalin
receptor
main physiologic effect
mu delta
analgesia
Dynorphins A&B
receptor
main physiologic effect
K
analgesia
ACTH
receptor
main physiologic effect
MC2R
adrenal stimulation
Mu 2 effects
4 Unfavorable
bradycardia
respiratory depression
constipation-inhibit GI motility
miosis
B endorphin how many AA
31
Dynorphin A&B how many AA
13
Enkephalins how many AA
5
post transcriptional modification is ?
alternate splicing of receptor mRNA to make subtypes
mu 1,2,3
post translational modification is
the way we make our endogenous opioids from big precursor proteins
each precursor has separate gene and separate mrna
MAPK cascade is activated leading to
gene expression and neuroplasticity which leads to addiction, tolerance, and opioid induced hyperalgesia
opioids cause what in the cerebrum
sedation
opioids cause what in the supraspinal (central)
truncal rigidity
Respiratory depression is a result of activation of mu receptors where
brain stem respiratory center
Hypoxic drive is ____by opioids
decreased
Apneic threshold is _____by opioids
increased
higher CO2 level required to take a breath
