Lesson plan

CI-1017

CI-1017 is a muscarinic acetylcholine receptor agonist which is selective for and is approximately equipotent at the M 1 and M 4 receptors, with 20-30-fold lower affinity for the M 2 , M 3 , and M 5 subtypes It is the (R)-enantiomer of the racemic compound PD-142,505. In animals CI-1017 improves learning and memory and increases the electrical activity of the hippocampus through activation of the M 1 receptor, while minimally producing parasympathetic side effects and only at very high doses. It also inhibits production of amyloidogenic A beta peptide and increases secretion of soluble amyloid precursor protein via stimulation of the M 1 receptor as well. Based on these data, it was hypothesized that CI-1017 could not only treat the symptoms of Alzheimer's disease, but could also potentially slow disease progression. It was tested in clinical trials for this purpose in the early 2000s but was abandoned due to lack of efficacy.

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Article summary

CI-1017 is a muscarinic acetylcholine receptor agonist which is selective for and is approximately equipotent at the M 1 and M 4 receptors, with 20-30-fold lower affinity for the M 2 , M 3 , and M 5 subtypes It is the (R)-enantiomer of the racemic compound PD-142,505. In animals CI-1017 improves learning and memory and increases the electrical activity of the hippocampus through activation of the M 1 receptor, while minimally producing parasympathetic side effects and only at very high doses. It also inhibits production of amyloidogenic A beta peptide and increases secretion of soluble amyloid precursor protein via stimulation of the M 1 receptor as well. Based on these data, it was hypothesized that CI-1017 could not only treat the symptoms of Alzheimer's disease, but could also potentially slow disease progression. It was tested in clinical trials for this purpose in the early 2000s but was abandoned due to lack of efficacy.

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Discussion questions

  1. Summarise the article in your own words. Which single claim would you verify first, and why?
  2. Which claim in this article is most likely to be revised as the sources update? How would you check its current status?
  3. If two sources disagreed about one of these facts, what would you need in order to trust one over the other?

Bibliography

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Key claims and bibliography are generated from the same tracked claims and sources as the article page.