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20 Cards in this Set
- Front
- Back
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The alpha 1 receptor is a ___ GPCR and mediates [organ action] when stimulated.
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Gq
smooth muscle contraction |
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The alpha 2 receptor is a ___ GPCR and mediates [organ action] when stimulated.
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Gi
NT inhibitor, cardiac muscle relaxer |
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The beta 1 receptor is a ___ GPCR and mediates [organ action] when stimulated.
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Gs
Cardiac muscle contractor |
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The beta 2 receptor is a ___ GPCR and mediates [organ action] when stimulated.
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Gs
Smooth muscle relaxer |
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The beta 3 receptor is a ___ GPCR and mediates [organ action] when stimulated.
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Gs
Fat cell lipolysis |
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Nicotinic Acetylcholine Receptors -- where and what kind?
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Ionotropic / ligand-gated ion channel on skeletal muscle
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Acetylcholine -- synthesis and degradation
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Choline + AcetylCoA -----(aceteyltransferase) --- > Acetylcholine + CoA in nerve terminal
Acetylcholine + ACh esterase ----> choline + AcetylCoA at NMJ |
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Muscarinic AC Receptors
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Metabotropic, GPCRs on the heart and smooth muscle and sweat glands
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Name 2 non-selective beta-blockers
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Alprenelol (Gubernal®)
Pindolol (Visken®) Propranolol (Inderal®) Sotalol (Betapace®) Timolol (Blocadren®) |
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Name at least 2 beta-1 specific blockers.
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Acebutolol (Sectral®)
Atenolol (Tenormin®) Betaxolol (Betoptic®) Esmolol (Brevibloc®) Metoprolol (Lopressor®) |
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Name the three subtypes of calcium channel antagonists
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Phenylakylamines (PHA)
Benzothiazepines (BNZ) Dihydropyridines (DHP) |
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What do calcium channel antagonists do?
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Inhibit L-type Ca2+ channels in myocardium and VSM.
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What do beta blockers do?
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Lower heart rate, lower cardiac output, reduce preload/afterload, lower oxygen demand
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What's an example of PHA?
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Verapamil
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What's an example of BNZ?
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Diltiazem
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What's an example of a dihydropyridine (DHP)?
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Amlodipine
Nicardapine |
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What Calcium channel subtype affects the heart the strongest?
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PHA > BNZ >>> DHP
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What Calcium channel subtype affects the VSM the strongest?
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DHP >>> PHA=BNZ
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Mechanism of action of Ca+ channel blockers on heart.
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↓Ca2+ influx during cardiac AP → ↓ conduction velocity → ↓ HR → ↓ CO → ↓ myocardial O2 demand
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Mechanism of action of Ca+ channel blockers on VSM.
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↓Ca2+ influx following GPCR activation → ↓ MLCK activity → ↓ vascular tone → ↓ afterload
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