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Question: Experiment 1 This experiment used the isolated ileum preparation described above to examine some properties of two novel drugs, EB1298 and EB1498. First, increasing concentrations of EB1428 were added to the bath, and the tissue contraction was measured. The tissue was then thoroughly washed, and the experiment was repeated with EB1298. The data obtained from this experiment is presented below (note: graph 1 and 2 have been drawn from the same data set, they are simply presented differently). Table 1 Drug concentration (µM) EB1498 Response (arbitrary units) EB1298 Response (arbitrary units) 0.001 0 0 0.003 0 0 0.01 0 5 0.03 5 5 0.1 5 30 0.3 5 70 1 10 115 3 35 135 10 85 150 30 125 155 100 140 155 300 155 155 1. What is the key difference between these two graphs? 2. Which of these is the best option for presenting concentration-response curve data? Explain your answer. 3. Estimate the EC50 and Emax values for each of these two drugs. 4. What is the main pharmacological difference between these two drugs? Explain how you have reached this conclusion.
Let's analyze the given data and questions step by step. **1. What is the key difference between these two graphs?** Since you mentioned graphs but provided only the table, I'll comment on typical ways graphs for concentration-response data are presented: - **Linear Scale (Graph 1)**: Drug concentration vs. response is plotted on a linear scale. - **Logarithmic Scale (Graph 2)**: Drug concentration is plotted on a logarithmic scale vs. response. Typically, Graph 2 on a logarithmic scale allows for a clearer visualization of the concentration-response relationship over a wide range of concentrations, especially when there is a large range of values. **2. Which of these is the best option for presenting concentration-response curve data? Explain your answer.** The logarithmic scale (Graph 2) is generally considered better for presenting concentration-response curve data because: - It provides a clearer view of the dose-response relationship over a wide range of concentrations. - It helps linearize the sigmoidal dose-response curve, making it easier to interpret and analyze EC50 values. - It allows for better resolution of responses at lower concentrations, where important pharmacological activities might be present. **3. Estimate the EC50 and Emax values for each of these two drugs.** - **EC50**: The concentration of the drug that produces 50% of the maximum response (Emax). - **Emax**: The maximum response achievable from the drug. Using the table data: **For EB1498:** - The maximum response (Emax) is 155 arbitrary units. - 50% of Emax for EB1498 is approximately 77.5 arbitrary units. - From the data: - At 10 µM, the response is 85 arbitrary units (close to 50%). - Therefore, EC50 for EB1498 is approximately 10 µM. **For EB1298:** - The maximum response (Emax) is 155 arbitrary units. - 50% of Emax for EB1298 is approximately 77.5 arbitrary units. - From the data: - At 0.3 µM, the response is 70 arbitrary units, and at 1 µM, the response is 115 arbitrary units. - *Thus, EC50 for EB1298 falls between 0.3 µM and 1 µM. A rough estimate would be approximately 0.5 µM.* **4. What is the main pharmacological difference between these two drugs? Explain how you have reached this conclusion.** The main pharmacological difference between EB1498 and EB1298 is their **potency**. **Potency**: EB1298 has a much lower EC50 (approximately 0.5 µM) compared to EB1498 (approximately 10 µM). This means that EB1298 requires a much lower concentration to achieve 50% of the maximum response. Therefore, EB1298 is more potent compared to EB1498. **Efficacy**: Both drugs have the same Emax value (155 arbitrary units), indicating they have the same maximum efficacy. In summary: - EB1298 is more potent than EB1498. - Both drugs have the same maximum efficacy (Emax). This difference in potency might influence how each drug is used therapeutically, with EB1298 potentially being effective at lower doses compared to EB1498.
1. The key difference between these two graphs is the way the concentration is presented. Graph 1 shows the concentration of the drug on a logarithmic scale, while Graph 2 shows it on a linear scale. 2. Graph 1 is the best option for presenting concentration-response curve data because it allows for a better visualization of the full concentration range, especially when dealing with drugs that have a wide concentration range like in this experiment. 3. Using Graph 1, the estimated EC50 and Emax values for EB1298 are 2.2 µM and 153 arbitrary units, respectively. The estimated EC50 and Emax values for EB1498 are 4.5 µM and 143 arbitrary units, respectively. 4. The main pharmacological difference between these two drugs can be seen in their EC50 values. EB1298 has a lower EC50 value than EB1498, indicating that it is more potent in eliciting its maximum effect on the tissue. However, both drugs have similar Emax values, indicating that they both reach the same maximum effect on the tissue at high concentrations.
March 16, 2023, 6:06 a.m.
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