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Adrenergic Agonists
Neuro 3 Pharm
20
Pharmacology
Graduate
06/06/2011

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Cards

Term
Synthesis pathway
Definition
tyrosine --> L-Dopa --> Dopamine --> Norepi --> Epi
Term
Enzymes involved in metabolism
Definition
MAO and COMT
Term
Enzymes altering re-uptake
Definition
Dopamine Transporter (DAT)
Norepinephrine transporters (NET)- tricyclic antidepressants block this
Term
Amphetamine
Definition
Block reuptake and reverse the transporter- lots of catecholamine release
Term
alpha- 1- AR
Definition
- 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
Term
Phenylephrine
Definition
- agonist for alpha1AR
Term
alpha-2-AR
Definition
- 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
Term
Clonidine
Definition
- alpha2AR agonist
- for hypertension because it decreases BP
Term
Oxymetazoline
Definition
- alpha2AR agonist
- apply topically for congestion
Term
apraclonidine
Definition
- alpha2AR agonist
- apply topically for glaucoma
Term
Beta1AR
Definition
- 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
Term
Dobutamine
Definition
B1AR agonist
- increases cardiac output with less reflex tachycardia than non-selective B agonists
Term
beta2AR
Definition
- 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)
Term
Albuterol
Definition
- B2AR agonist
- Use for asthma
Term
Terbutaline
Definition
- B2AR agonist
- Use for acute bronchospasm and premature labor
Term
Salmeterol
Definition
- B2AR agonist
- chronic bronchospasm
Term
beta3AR
Definition
- least understood, may stimulate lipolysis
- seems to be involved in heart failure
- relaxes detrusor muscles in bladder
Term
Bromocriptine
Definition
- agonist for D2
Term
Arrestins
Definition
- 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)
Term
Cocaine
Definition
- blocks reuptake of dopamine via DAT
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