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32 Cards in this Set
- Front
- Back
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what is a graded response curve
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experiment on one person or cells that measures dose on x axis and response on y axis
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what is Kd
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binding constant of drug
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what is a probit plot
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a dose-response curve using a log scale that makes the best fit line for dose response data
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what is Emax
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efficacy; maximum response achieved by agonist
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what is ED50
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potency: drug concentration at which 50% of Emax is achieved
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what is one reason for partial agonist weaker response compared to full agonist
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maybe it doesn't cause as much signal transduction.
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what do partial agonist curves look like for dose response compared to full agonists
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less potency and less efficacy
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what is a quantal response
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you look at all or nothing response in a whole bunch of people. x axis has dose. y axis has number of people affected. normal distribution typical
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what is therapeutic index
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LD50/ED50. bigger TI = safer
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what are the three types of ion channel effects can drugs have
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hit the ligand site to open up the channel (e.g GABA-gated Cl channel), blocker, modulator (don't bind to site of typical ligand, can keep channel open longer, can change the channel's affinity for its receptor)
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how does Kd relate to drug potency
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Kd is a measure of affinity. different ligands have different Kd and this affects drug potency
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intrinsic activity
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measure of ability of bound drug to activate the receptor. distinguishes agonist from antagonist
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what are four different types of receptors
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1. channel-linked receptors (ionotropic)
2. G-protein coupled receptors (metabotropic) 3. kinase-linked receptors 4. receptors linked to gene transcription (nuclear receptors) |
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what is the time course for effectiveness of these different receptors.
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1. channel-linked receptors (ionotropic): ms
2. G-protein coupled receptors (metabotropic): seconds 3. kinase-linked receptors: minutes 4. receptors linked to gene transcription (nuclear receptors): hours |
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what affect do channel-linked receptors have
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hyperpolarization or depolarization
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what effect do GPCR have
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G protein can act on PM ion channels to change excitability. G protein can act on PM protein. membrane protein then acts on second messengers. these second messengers can cause Ca2+ release, protein phosphorylation, or other things to occur
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what type of receptor is a Nicotinic ACh receptor
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channel-linked receptor (ionotropic)
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what type of receptor is muscarinic ACh receptor
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GPCR
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what are the different membrane target enzymes for GPCR
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guanylate cyclase (cGMP), adenylate cyclase (cAMP), phospholipase C (IP3 = Ca release and DAG = PKC), phospholipase A2 (AA)
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Gs does
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activates Ca2+ channels, activates adenylyl cyclase
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Gi does
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activates K+ channels, inhibits adenylyl cylcase
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Go does
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inhibits Ca2+ channels
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Gq aka G11 does
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activates phospholipase C
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G12/13
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diverse ion transporter interactions
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mechanism of B1 and B2 adrenergic receptors
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Gs, activate Ca2+ channels and adenylyl cyclase (which makes cAMP which activates protein kinase A and Ca2+ channel opens. PKA phosphorylates target proteins)
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mechanism of alpha 2 adrenergic receptors
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Gi, activate K+ channels and inhibit adenylyl cyclase (which makes cAMP which activates protein kinase A and Ca2+ channel opens. PKA phosphorylates target proteins)
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mechanism of muscarinic m2/m4 cholinergic receptors
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Gi, activate K+ channels and inhibit adenylyl cyclase (which makes cAMP which activates protein kinase A and Ca2+ channel opens. PKA phosphorylates target proteins)
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what are M1, M3, and M5 signal transduction pathways
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Gq/G11. activate PLC (increase IP3 and DAG which increase Ca2+ and PkC). depolarization (increase EPsP) activate PLD2. activate PLA2 (increase arachidonic acid)
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what are M2/M4 signalling pathways
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Gi/Go. inhibit Ad Cyl (decrease cAMP). activate K_ channels, inhibit Ca2+ channels. hyperpolarization and inhibition
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what is the nicotonic receptor signaling pathway
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once ACh binds they let in Na+ and let out K+
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what do alpha 1 receptors do
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Gs that activates PLC (increase IP3 and DAG which increase Ca2+ and PkC)
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