The potency of agonists is frequently defined in terms of their affinity and theirefficacy. Explain what these two terms mean. Use diagrams to illustrate your answer
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- Estimate the binding affi nity of a ligand for its receptor from the followingdata:The Structure of the acetylcholine receptor is shown below: A. Knowing the amino acid sequence of this protein, what tool would you use to identify the membrane-spanning region? Explain how it works.The drug Buckeyium binds to the NMDA receptor at the orthosteric binding site (were glutamate would normally bind). Assume that glycine is already bound, and that magnesium is not blocking the NMDAR ion channel. If the channel does not open as a result of Buckeyium binding than Buckeyium would be considered a
- The catechol system is important for the binding of adrenergic agonists, yet is not required for adrenergic antagonists. Why should this be the case? The active enantiomer of arylpropanolamines is S, yet for the arylethanolamines it is R. What do you think is going on in the binding site? Summarize what a selective noradrenaline reuptake inhibitor does and how it would affect depression.Buckeyium is a medication that binds to the NMDA receptor at the orthosteric binding site (were glutamate would normally bind). Assume glycine is already bonded and magnesium isn't inhibiting the NMDAR ion channel. Buckeyium would be regarded a poison if the channel did not open as a consequence of its binding.A common membrane-bound intermediary between the receptor and the effector protein within the plasma membrane is the __________________.
- An investigator is studying the electrophysical properties of gastrointestinal smooth muscle cells using microelectrodes. He measures the resting membrane potential of a cell to be -70 mV. The equilibrium potentials of different ions involved in generating the membrane potential are shown. ENa Ek Eca EM² Ecr +65 mV -85 mV +120 mV +10 mV -85 mV Which of the following is the most important contributor to the difference between the resting membrane potential and the equilibrium potential of potassium?Organophosphate poisoning is a result of excess acetylcholine at different nerves and receptors in the body because acetylcholinesterase is blocked. Please provide rational to explain how the binding of organophosphate with serine in the acetylcholinesterase enzyme leads to excess accumulation of acetylcholine.you have been asked to develop a drug that could inhibit an enzyme linked receptor. what are the potential pharmacological targets you could design your drug to interact with. which one should you choose and why
- An antibody has been isolated that binds to F-actin but not to G-actin. Whatstructural feature(s) of F-actin do you suppose the antibody binds (i.e., howis the antibody able to distinguish between these two forms of actin)?FRAP is a technique used to determine the mobility of a molecule in a membrane. Design a FRAP experiment to test the mobility of an insulin receptor. Would you expect the receptor to be more mobile before or after insulin binding?Tyrosine came from the Greek word "tyros" which means cheese as it was discovered in cheese by Justus von Liebig, a German chemist in 1846. Tyrosine serves as the precursor for dopamine - the neurotransmitter which is considered as the "reward or pleasure molecule" in our brain. It is also involved in controlling the fine motor movement of our muscles such as those of our hands. Draw the titrimetric profile of tyrosine and calculate its isoelectric pH. [Note: The aromatic hydroxyl group is titratable]