Pharmacology lecture 3

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What does a graded dose response relationship show?
A response of a particular system
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What does a quantal dose response relationship show?
The drug dose required to produce a specified response determined in each member of a population
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What does a dose-response curve allow you to estimate?
1) Emax 2) Concentration or dose required to produce 50% of maximal response - EC50
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What does a dose-response curve allow you to determine? And define them.
1) Efficacy - ability to produce a desired response 2) Potency - amount required to produce a max effect
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Kd = (definition)
concentration of ligand at which 50% of available receptors are occupied(equilibrium dissociation constant)
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Kd = (formula)
Kd = K-1/K1
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Affinity = (formula)
Affinity = K1/K-1
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A LOWER Kd indicates....
a tighter ligand-receptor interaction (HIGHER AFFINITY)
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A LOWER EC50 value....
the GREATER the POTENCY
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FULL agonist
High efficacy - produce MAX response while occupy small % of receptors
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PARTIAL agonist
Low efficacy - unable to produce a max response even when occupying all available receptors
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Tachyphylaxis
Desensitisation of receptors
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What do positive allosteric modulators do?
Not active alone but INCREASE affinity and/or efficacy of endogenous agonist
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What do negative allosteric modulators do?
Not active alone but DECREASE affinity and/or efficacy of endogenous agonists
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What does a quantal dose response relationship show?

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The drug dose required to produce a specified response determined in each member of a population

Card 3

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What does a dose-response curve allow you to estimate?

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Card 4

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What does a dose-response curve allow you to determine? And define them.

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Card 5

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Kd = (definition)

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