Opioid receptors
Where do Mu opioid receptors work?
Are responsible for analgesia in the spinal and supraspinal areas specifically the substantia gelatinosa also in the posterior horn of the spinal
Mu1- MUSE
Miosis Urinary retention Supraspinal analgesia Europhia
What opioids are agonists on all three receptors
Morphine Meperidine Fentanyl Sufentanil Alfentanil Remifentanil
Which opioid causes euphoria?
Mu1
synthetics opioids act on what receptor
Mu1 and Mu2
Endorphins and morphine are associated with which receptor
Mu1 and mu2
Which Opioid receptor causes marked constipation?
Mu2
What are opioid antagonist on all three receptors
Naltrexone Naloxone Nalmefene
What opioids Are antagonists on the Mu receptor
Naltrexone Naloxone Nalmefene
MU receptors have a different sub time. At this time the significance is not well understood. True or false
True
Opioid receptors either act to inhibit Adenylyl cyclase and cyclic adenosine monophosphate cAMP production or they directly interact with different ion channels in the membrane.
True
Once activated, opioid receptors can cause
attenuation of the excitability of neurons and or reduces the release of pronociceptive neuropeptides:
How many opioid receptors are there?
3. Mu, Kappa and Delta
What percentage of transmembrane G protein coupled receptors show homologies for opioid genes?
40-70%
Mu2- Brains
Bradycardia Respiratory depression Itching Nausea and vomiting and constipation Spain also analgesia
What opioids or partial agonist on the Kappa receptor
Butorphanol Nalbuphine
What receptors are agonists on the Delta receptor
Butorphanol Nalbuphine
Enkaphalins and urinary retention is associated with which opioid receptor?
Delta
Physical dependence and respiratory depression is seen in which opioid receptor?
Delta
What are the names of naturally occurring opioid agonist
Endorphins Enkephalins Dynorphins
All opioid receptors are ________.
G-protein coupled
Where can opioid receptors modulate?
In the pre-and post synaptic membrane, calcium channels by suppressing calcium influx
What occurs when G Protein receptors opens after being activated by an opioid receptor
It results in an increase in potassium entering the cell which prevents neural excitability and Prevents action potential
dynorphins and diureses is associated with which receptor
Kappa Agonists
Does kappa receptors cause respiratory depression
Kappa receptors are not associated with respiratory depression but they do cause G.I. motility and dysphoria
Delta- Raps
Respiratory depression Addictive Poorly understood and constiPation Supraspinal
What does mu receptors activation cause?
Respiratory depression, decreased GI motility
Opioids classifications by Chemical class
See table 11.1 page 129
Kappa- same shit different day man!
Spinal and supraspinal analgesia Sedation Dysphoria and diuresis Dependence Miosis
Where are opioid receptors expressed?
They are expressed in the central and peripheral neurons, Adrenal pituitary immune and ectodermal cells
Where are the kappa receptors located?
They are located in the same area as the MU receptors
What are delta receptors responsible for
They are responsible for supraspinal and spinal analgesia. Their activation causes modulation of hormone a neurotransmitter release.
