(5 points) Based on the Ko values which of these drugs is the tightest binder to
ID: 269819 • Letter: #
Question
(5 points) Based on the Ko values which of these drugs is the tightest binder to y-opioid Louw a.cr,'^?? (5 points) Based on the Ko values, which of these drugs is the weakest binder receptors? (5 points) Naltrexone is an antagonist that can be used to reve Naltrexone be effective for reversing a Carfentanil overdose? It so, under what conditions? es (3) Short Answer (25 points) (10 points) Give two examples of changes that can occur in the Nucleus Accumbens as a result of addiction. c pamine ??teas 2.Explanation / Answer
We are taking about class of drugs called opiate analgesics which bind to mu opiate receptors which are cell membrane bound G protien coupled receptors. This is just a brief idea.
The drugs list to choose from is not seen in the question. However, the approach will be that the binding affinity of opiate drug to opiate receptors is represented by its Kd value. A high Kd value means low affinity and vice versa.
So, if we know the Kd values of the drugs we can easily say which drug will be tighlty bound and whichwill be loosely bound to its receptor.
Carfentanil is an analogue of the drug fentanyl. Naltrexone is an effective antagonist for Carfentanil.100mg Naltrexone / mg of Carfentanil antagonizes the effect of Carfentanil. Naltrexone is effective in patients who wish to withdraw use of opoids, in their very first stage of treatment.
Nucleus Accumbens is an area in forebrain associated with desire, satiety and inhibition. You can say that is the reward centre and hence a major contributor in the formation of addiction to drug abuse. Examples of changes in Nucleus Accumbens as a result of addiction are:
1. Addictive drugs induce the release of dopamine into Nucleus Accumbens that increase the urge for drug eventually leading to habitual use and then addiction.
2. Dopamine then interacts with glutamate, another neurotransmitter of the brain, to aid in reward learning on consuming the drug. Repeated exposure to drug thus weaken the connections with Nucleus Accumbens whcih ultimately leads to hijack of the brain for repeated urge to consume the drug of abuse.
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