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Pharmacodynamics
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mexico-robert-magazine-bakerloo-single-ack
Status
Last Update
Fields
Published
08/12/2024
Pharmacodynamics
Published
08/12/2024
Receptors:
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08/12/2024
Effectors
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08/12/2024
Low Kd = {{c1::High Affinity}}
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Receptors The majority of all Receptors are {{c1::proteins }}Receptors bind with drugs and bring about a change in cell {{c1::function}}
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Evidence for Receptors
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{{c1::Agonist}} can “turn on” an intracellular amplification system (efficacy)
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{{c1::Partial Agonist}} binds with reduced amplification (decreased efficacy) in comparison to a full agonist
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08/12/2024
{{c1::Antagonist}} binds the receptor without “turning on” the intracellular system. Blocks agonist from binding to receptor
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Gs stimulates {{c1::adenylate cyclase}} → {{c1::increases}} cAMP and PKA → change {{c1::gene transcription}} → ind…
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Gi inhibits {{c1::adenylate cyclase }}→ {{c1::decrease}} cAMP and PKA → change {{c1::gene transcription}} → indirectly alter&…
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Gq → increase {{c1::phospholipase C (PLC)}} activity → breaks down {{c1::PIP2}} into {{c1::IP3 and DAG}} → {{c1::IP…
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G-protein coupled to {{c1::phospholipase A2 (PLA2)}} pathway → arachidonic acid release
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Affinity is the ability for binding, due to s{{c1::hape, size, charge, atomic composition }}
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Give evidence for the existence of receptors.
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Ligand gated ion channel
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G-Protein Coupled Receptors
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Kinase Receptors
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Nuclear Receptors
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{{c1::Potency}}: dosage/concentration required to induce/block a response
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{{c1::Efficacy}}: measure of drug’s ability to induce a response
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{{c1::Competitive antagonist}}: reversible binding so agonist can compete for the receptor → increased agonist concentration can push off competitive …
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{{c1::Noncompetitive antagonist}}: irreversible (covalent) binding so agonist cannot push off antagonist → causes loss of efficacy
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If there are spare receptors, EC50 {{c1::<}} Kd
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Define signal transduction
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Describe how a G-protein can influence gene transcription
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Describe how a G-protein can alter ion channel activity.
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Tyrosine kinase: binding → {{c1::dimerize}} (conformational change) → {{c1::phosphorylation}} → {{c1::activation of kinase cascade…
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08/12/2024
Corticosteroid receptors (nuclear receptors): Bind in {{c1::cytoplasm or nucleus}} → enters nucleus → {{c1::alter gene transcription }}…
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Dose-Response Curves
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{{c1::ED50}} - median effective dose = dose at 50% response {{c1::LD50}}- median lethal dose {{c1::TD50}}- median toxic dose for a part…
Published
08/12/2024
Status
Last Update
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