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| An agonist can be defined as '''a drug that binds to a target molecule and results in activation of the receptor and thus a tissue response'''. | | An agonist can be defined as '''a drug that binds to a target molecule and results in activation of the receptor and thus a tissue response'''. |
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− | * An agonist forms a complex with the receptor. This complex is '''dynamic''' as the agonist will continously dissociate and associate with the receptor. The agonist will continue to do this and thus producing a response, until the concentration of the agonist is reduced to a level at which no tissue response occurs. | + | * An agonist forms a complex with the receptor. This complex is '''dynamic''' as the agonist will continously associate and dissociate with the receptor. The agonist will continue to do this and thus produce a response, until the concentration of the agonist is reduced to a level at which binding no longer occurs. |
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− | * The rate of complex fromation is dependent on two factors: '''agonist concentration''' and the '''number of free receptors'''. | + | * The rate of complex formation is dependent on two factors: '''agonist concentration''' and the '''number of free receptors'''. |
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− | * The '''affinty''' of a drug to a receptor varies and can be compared using the '''equilinbrum constant or K<sub>A</sub>'''. | + | * The '''affinity''' of a drug to a receptor varies and can be compared using the '''equilibrium constant or K<sub>A</sub>'''. |
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| This can be defined as the concentration of a drug which results in 50% of receptors being bound in equilibrium or when '''K<sub>1</sub>=K<sub>-1</sub>'''. | | This can be defined as the concentration of a drug which results in 50% of receptors being bound in equilibrium or when '''K<sub>1</sub>=K<sub>-1</sub>'''. |
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| <big>'''Drug + Number of Free Receptors = Drug-Receptor Complexes'''</big> | | <big>'''Drug + Number of Free Receptors = Drug-Receptor Complexes'''</big> |
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− | Where '''K<sub>1</sub>''' is the rate constant in a forward direction | + | Where '''K<sub>1</sub>''' is the rate constant in a forward direction (association rate constant) |
− | and '''K<sub>-1</sub>''' is the rate constant in a backward direction | + | and '''K<sub>-1</sub>''' is the rate constant in a backward direction (dissociation rate constant) |
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| Therefore a drug that has a higher affinity to a receptor has a lower '''K<sub>A</sub>''' value. | | Therefore a drug that has a higher affinity to a receptor has a lower '''K<sub>A</sub>''' value. |
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| * By an intracellular second messenger system | | * By an intracellular second messenger system |
| * By DNA transcription | | * By DNA transcription |
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| ==Antagonists== | | ==Antagonists== |