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Effects of activation
of opiate receptors
and drugs acting on
them
Aron Takacs
Opioid Receptors
•
G protein-coupled receptors
•
Activated by opioid peptides
•
Mainly found in:
 Brain
 Spinal cord
 Digestive Tract
•
Main types:




Delta opioid receptor
Kappa opioid receptor
Mu opioid receptor
Nociceptin opioid receptor
Mu receptor bound to antagonist
Opiates
•
Types:
 Agonist
 Antagonist
•
Endogenous opioids:




Dynorphins
Enkephalins
Endorphins
Nociceptin
nociceptin
Effects of activation of opiate
receptors
•
Analgesia = Pain killer
•
Sedation
•
Reduces the excitability of neurons
•
Can create strong physical addiction
•
GABA inhibition mechanism:
 Suppresses the release of GABA
 GABA regulates the release of dopamine
 Increases dopamine levels
morphine
Drugs
•
Morphine:




•
Binds to Mu and Delta receptors
Analgesia
Sedation
Standard against all other opiates
Heroin:
 2-4x more potent then morphine
 Used in the past as
 cough medication
 antidiarrheal
 cocaine addiction medication
heroin