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15 Cards in this Set
- Front
- Back
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What is potency?
What is efficacy? |
Potency - concentration of drug required to achieve a certain effect (usually references to EC50)
Efficacy - magnitude of the drug's action at the limit of its concentration (Emax) |
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What is a receptor?
Agonist? Antagonist? |
Receptor - protein that binds a signaling molecule and, in doing so, generates a signal of its own
Agonist - a molecule that "activates" a receptor (full, partial) Antagonist - a molecule that prevents activation of a receptor by an agonist (neutral, inverse) |
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What are the 5 transmembrane signaling mechanisms?
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1. A lipid soluble signal crosses plasma membrane and acts on INTRAcellular receptor
2. Signal binds EC domain, activates enzymatic activity of receptor 3. Tyrosine-Kinase Receptor 4. Ion channel 5. GPCR receptor |
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What type of signaling mechanism do cytokine receptors utilize?
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Signal binds to EC domain or receptor, activating enzymatic activity.
Uses JAK-STAT system JAK kinase gets activated, phosphorylates STAT which is a transcription factor |
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What type of signaling mechanism does EGF utilize?
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Tyosine Kinase receptor
- Upon binding, receptor goes from inactive monomer to active dimer |
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What type of receptor is a Nicotinic Receptor?
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Ligand-gated ion channel
- When ACh binds, allows Na+ ions to flow into neuron |
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What is the configuration of a GPCR?
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Heterotrimeric (a, b, g) configuration
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What is the mechanism of action of a GPCR?
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- Agonist binds
- Activated G-Protein - G-Protein changes activity of effector element (adenyl cyclase, ion channel) - Element changes concentration of second messenger (cAMP, Ca+2) |
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What are the 3 different subtypes of GPCRs and what do they do?
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Gs - Adenylyl Cyclase (stimulation of cAMP)
Gi - Adnenylyl cyclase (inhibition of cAMP) Gq - PLC-Beta (stimulation Ca+2) |
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What is an example of a Gs receptor?
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Actions of epinephrine through the Beta1-adrenergic receptor in the LUNGS
- produces cAMP as second messenger |
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What is an example of a Gi receptor?
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Actions of Ach through the M2 muscarinic receptor
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What is histamine's effect on Bronchiolar smooth muscle?
Vascular Smooth muscle? Why? |
Bronchiolar - contraction
Vascular - relaxation Different responses because different H receptors (Bronchiolar - Gq, Vascular - Gs) |
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What is epinephrines effect an Cardiac myocytes?
On Bronchiolar smooth muscle? What specific receptors do both use? |
Cardiac - contraction (via B1 receptor) Gs
Bronchiolar - relaxation (via B2 receptor) Gs Different signaling pathways |
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What do histamine blocker allergy meds sometimes cause drowsiness?
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Because they can cross stimulate similiar receptors that cause drowsiness
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What is the mechanism of GPCR desensitization?
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- Serine residues in GPCR tail are phosphorylated by GPCR kinases (GRKs)
- This recruits B-arrestin - B arrestin decreases receptor ability to interact with G-Protein subunit |
