PCL201H1 Lecture Notes - Lecture 2: Irreversible Antagonist, Diazepam, Fluoxetine

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11 Jan 2018

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Determine time course for drug after administration
Linked to PD by plasma concentration
Interaction with target
Reversible via weak chemical bonds
Irreversible require new synthesis of target
Concentration range (saturable at high, no response at low)
Desired specificity, chemical specificity (twice dose in racemic mixture)
Can be inhibited
Response is relative to drug concentration, intrinsic activity and number of receptors
Changes in signaling
Receptors participate in intracellular communication via chemical signals
Drugs are like ligands
Effectors are activated by signaling cascade
Adenylyl cyclase: increases cAMP
Physiological effect
Dose-response curve (acute response dissipates over time)
Semi-logarithmic: expands conc. scale at low, compresses at high
Efficacy: ability to give effect
Emax: maximal response
EC50: drug conc. at 50% of max response (POTENCY)
ED *effective dose
Mimic or enhance action of endogenous compound
Binds at same site, full response
Salbutamol: mimics epinephrine at B2 activating GPCR
Pindolol: at B1, treat hypertension by blunting signalling
Positive Allosteric Modulator
Distinct site
Shift curve LEFT
Diazepam: PAM of GABA receptor that decreases neuronal activity
Pharmacological: Blocks ability of receptor-drug interaction by another ligand
Chemical: chelation, effect lost
Physiological: opposing effects
Zero efficacy on its own
Binds same site
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