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tyrosine --> L-Dopa --> Dopamine --> Norepi --> Epi |
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Enzymes involved in metabolism |
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Enzymes altering re-uptake |
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Dopamine Transporter (DAT) Norepinephrine transporters (NET)- tricyclic antidepressants block this |
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Block reuptake and reverse the transporter- lots of catecholamine release |
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- G protein stimulates PLC, making IP3, DAG, and increasing Ca - primarily located in vessels in skin and gut - activation causes contraction - don't need a lot of blood in skin and gut - also get contraction of: pupillary dilator muscle, heart, GU tract - Phenylephrine |
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- Inhibits AC, decreasing cAMP - direct opposition to betaAR? - when applied directly on vessel, it will contract - if given systemically, CNS sends out negative feedback leading to a decrease in heart rate and blood pressure - Overall decrease in norepi levels - peripheral actions: vasoconstriction when topical application, GI decreased secretion and motility, pancrease decreased release of insulin, decreased lipolysis, decreased aqueous humor production - Clonidine- decreases BP - oxymetazoline- topically for congestion - apraclonidine- topically for glaucoma |
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- alpha2AR agonist - for hypertension because it decreases BP |
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- alpha2AR agonist - apply topically for congestion |
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- alpha2AR agonist - apply topically for glaucoma |
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- GPCR that stimulates AC to make more cAMP - heart- stimulates rate and force of contractions - kidney- stimulates renin release by JGC's, renin increases BP - dobutamine- increases cardiac output with less reflex tachycardia than non-selective B agonists |
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B1AR agonist - increases cardiac output with less reflex tachycardia than non-selective B agonists |
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- GCPR stimulating AC to make cAMP - bronchi, uterus, bladder- relaxes vascular smooth muscle - cardiovascular- relaxes peripheral vascular resistance, so increases HR - skeletal muscle- increases potassium uptake (increasing contraction) - liver- stimulates glycogenolysis - pancreatic B cells- stimulates insulin release - Albuterol (asthma), terbutaline(acute bronchospasm, premature labor), salmeterol (chronic bronchospasm) |
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- B2AR agonist - Use for asthma |
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- B2AR agonist - Use for acute bronchospasm and premature labor |
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- B2AR agonist - chronic bronchospasm |
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- least understood, may stimulate lipolysis - seems to be involved in heart failure - relaxes detrusor muscles in bladder |
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- When GRK comes in and phosphorylates B2 receptor, arrestin comes in and internalizes this receptor - 2 possible outcomes: 1. resensitization 2. downregulated (not returned to surface) |
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Definition
- blocks reuptake of dopamine via DAT |
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