Someone recently bought our

students are currently browsing our notes.

X

Drug Receptor Interactions Notes

Pharmacology Notes > Drug Development (BIOL10822) Notes

This is an extract of our Drug Receptor Interactions document, which we sell as part of our Drug Development (BIOL10822) Notes collection written by the top tier of University Of Manchester students.

The following is a more accessble plain text extract of the PDF sample above, taken from our Drug Development (BIOL10822) Notes. Due to the challenges of extracting text from PDFs, it will have odd formatting:

e-learning III - Drug-Receptor Interactions
Potency - It is the concentration or dose of a substance required to give a specified effect. Often, we use the concentration or dose required to give 50% of the maximal effect. These terms have special names in pharmacology - EC 50 and ED50.
EC50 - The concentration of an agonist that gives 50% of the maximum response.
Kd - The equilibrium dissociation constant used to measure drug affinity. It is the concentration of a ligand that occupies 50% of a receptor population and thus as Kd increases, so affinity decreases.
pEC50 - The negative log of the EC50. For example, an EC50 of 1E-9 M gives a pEC50 of 9.
pKd - The negative log of the Kd. A drug with a Kd of 1E-9 M has a pKd of 9.
Sigmoid curve - An S shaped curve. Seen with log concentration response relationships.

Rectangular Hyperbola - A curve that rises and then smoothly reaches a plateau. Characteristic of concentration-response or concentration-binding relationships. Predicted by the Hill-Langmuir equation.

Bmax - The maximum binding obtained in a saturation assay. It corresponds to the number of receptors in the system.
Emax - The maximal effect that can be obtained from a functional assay. It may depend on both receptor and system factors.
Efficacy - The degree to which an agonist can activate a receptor. A full agonist has the maximal possible efficacy. An antagonist has zero efficacy. A partial agonist has some efficacy, but less than that of a full agonist.

Buy the full version of these notes or essay plans and more in our Drug Development (BIOL10822) Notes.