Introductory pharmacology
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- Created by: Alex
- Created on: 11-05-13 10:24
Pharmacology
Study of the effects of drugs on the function of living systems
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Drug
Any chemical substance with biological effects except nutrients - medicines, poisons, mind altering, mind-altering
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What drugs target
Mainly act on proteins. bind to/block receptors, ion channels, transporters & enzymes
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Receptors:
proteins which recognise and respond to a chemical signal
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Binding site
The point on the outside of the cell which the chemical bind to the receptor
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Functional site
The point on the outside of a cel that when a chemical binds to, the receptor causes a response inside the cell.
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Ligand
Chemical which binds to a receptor protein
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Agonist
Ligand which can activate a receptor
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Antagonist
liquid which blocks the effect of an agonist but has no effect on the receptor activation on its own
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Selectivity of Ligands
many are capable for more than 1 receptor type. similarities in molecular structure of ligands mediate selectivity of same receptor types. Drugs act specifically at low doses of selectively at high.
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Potency
amount(conc) of agonist needed to induce a given response. higher potency = lower dose needed for effect. potency determined by characteristics of receptor activiation
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Affinity
How effective a ligand binds to its receptor
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Efficiency
How effective a ligand activates its receptor to induce a response within the cell - agonist
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strength of receptor-ligand interaction determined by
electrical charge interactions, hydrogen bonding and hydrophobic interactions
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Law of mass action
predicts behaviors of solutions in dynamic equilibrium. rate of chamical reaction is proportional to the product of the concentrations of the reactants
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Receptor classification
Classified based on differences in how functional responses are induced with receptor binding
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Signal transduction
mechanism that converts a mechanical/chemical stimulus to a cell into a specific cellular response. Signal transduction starts with a signal to a receptor, and ends with a change in cell function.
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Ion channel
Protein channel in a cell membrane that allows passage of a specific ion down its concentration gradient. - don't have to go through hydrolipid ilayer. can be opened or shut
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Cation ion channel
positively charged ions
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Anion
Negatively charged ions
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Ion specific
Only a specific ion
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G-Protein coupled receptor
receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses
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G-Protein coupled receptor properties
most abundant type in the body. fast synaptic transmission. anchored by lipids in internal memberane. associated with GTP and GDP
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Structure of G-protein coupled receptors
trimeric structure - 3 protein subunits - alpha beta and gamma which bind to GDP and GTP
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G-protein receptor in resting state
G-protein subunit attatched to membrane in alpha-beta-gamma complex. GDP is bounf to alpha-subunit
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When agonist binds to G-protein receptor
GDP converted to GTP (P added by enzyme). Alpha-Beta-gamma complex dissociated forming an Alpha-GTP and Beta-Gamma complex
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GPCR inactivation
Activation of GTPase converts GTP-GDP. alpha-GDP combines with Beta-Gamma to form alpha-beta-gamma complex and reassociates with receptor in the membrane. GDP-alpha-beta-gamma complex ready again for GPCR activation.
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GPCR effectors - G proteins target 2nd messengers systems
Adenyl cyclase, phospholipase C and ion channels
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Adenyl Cyclase
Enzyme. forms cyclic 3'5' adenosine monophosphate (cAMP) from ATP. Phosphodiesterase turns cAMP to 5'AMP
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Gi effect on adenylyl cyclase
Inhibits - decrease cAMP levels
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Gs effect on adenylyl cyclase
stimulate - increases cAMP levels
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what do cAMP and protein kinases regulate function of?
Enzymes and ion channels
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Who the Agonist-Receptor-G-protein pathway works
Agonist binds to receptor. G-proteins are activated. Binds to adenyl cyclase. ATP->cAMP. either activates or inactivates protein kinases to produce different response.
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what does Phospholipase C form from PIP2?
inositol (1,4,5) trisphosphate - IP3 and diacylglycerol (DAG)
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effect of Gq on Phospholipase C
Stimulates, increasing IP3 and DAG
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Effect of Phospholipase C and IP3
Binds to IP3 receptor (ligand gated ca2+ channel on membrane of ER). IP3 increases intracellular Ca2+ opening channels & releasing Ca2+ from E.R into cell. Increased cellular Ca2+ activates protein kinases which regulate function of enzymes & ionchan
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Other cards in this set
Card 2
Front
Drug
Back
Any chemical substance with biological effects except nutrients - medicines, poisons, mind altering, mind-altering
Card 3
Front
What drugs target
Back
Card 4
Front
Receptors:
Back
Card 5
Front
Binding site
Back
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