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11 Cards in this Set
- Front
- Back
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Prolonged exposure and binding of ligand to receptor that leads to desensitization of the activated receptor where it does not respond to drug anymore
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Homologous Desensitization
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G Protein coupled receptor: G alpha stimulates
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Adenylyl cyclase
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G Protein coupled receptor: G beta gamma stimulates
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Phospholipase C
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THIS ACTION on the C-terminus of the Gprotein coupled receptor results in a decrease in ability for proteins to bind to the receptor --> Desensitization
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Phosphorylation causes Beta arrestin to attach to the receptor
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What phosphorylates the G protein coupled receptor?
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Beta adrenergic receptor kinase phosphorylates the receptor on the C-terminal
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Activation of a receptor causes a second messenger system that desensitize an unrelated class of receptors
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cross talk - heterologous desensitization
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How will heterologous desensitization be seen in a patient?
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Patient being treated with a series of medications can result in a diminished clinical response to a new drug upon first exposure - can incorrectly attribute it to genetic variability / enzyme metabolism
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How will homologous desensitization be seen in a patient?
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Tolerance or a diminished clinical response to a drug dose that was previously active
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Diminished or absent reponse to a drug or endogenous ligand
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Receptor Down regulation
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How do you have drug-induced receptor upregulation?
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Treat a patient with a drug receptor antagonist and receptors will up regulate and increase in density
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What disease is an example of induced upregulation
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Parkinson's disease has injury and death of dopamine neuron cell bodies in substantia nigra and has very little dopamine release from nerve terminals in the striatum. D2 receptors are up regulated to amplify signal
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