Corwin Mancuso

Homework 5

I searched for the structure under Markush as instructed. I further refined the search to

include only journal entries mainly due to the fact I used up all my PatentPak free trials. This

also allowed for more interesting articles to look through.

1. Hsu, J.C., Lin, J.Y., Hsu, M.Y., & Lin, P.C. (2018). Effectiveness and safety of immune

checkpoint inhibitors: A retrospective study in Taiwan. PLoS ONE, 13(8), n.p. (The

researchers worked for various pharmacological and medical departments at National

Cheng Kung University in Taiwan, one of the most prestigious universities in the nation.)

This article pertained to the three immune checkpoint inhibitors iplilimumab (CTLA-4),

nivolumab (PD-1), and pembrolizumab (PD-1) and how effective they were in treating multiple

types of aggressive cancers in Taiwanese patients, as well as prevalence of their side effects. It

was found that on average, most patients who died did so before the median overall survival rate

found in other studies; fatigue, rashes, and nausea were the most common side-effects. This

study was performed to provide the Taiwanese FDA and National Health Insurance with survival

statistics pertinent to Taiwanese patients

2. Zhang, T., Zheng, X., Wang, X., Zhao, H., et al. (2018). Maternal exposure to PM2.5

during pregnancy induces impaired development of cerebral cortex in mice offspring.

International Journal of Molecular Sciences, 19(1), 257/1-257/17. (All researchers were

 affiliated with various medical departments at Weifang Medical University in China,

apart from the statistician Hua Shen who hailed from the Department of Math and

Statistics at the University of Calgary.)

This article did not explicitly seem to pertain to the molecule in question, but rather to the

effect of air pollution on gestation and infant brain development in mice. Exposure to high

concentrations of small pollutant particulate matter suggested a significant detrimental effect on

infant cell apoptosis as well as smaller neuron size and decreased cytoplasm. Furthermore, the

maternal mice showed signs of anxiety, depression, and decreased performance in open field

experiments.

3. Farhan, M. & Perveen, M. (2017). Anxiolytic and antidepressant like profile of

repeatedly administrated escitalopram in behavioral animal models. Pakistan Journal of

Pharmaceutical Research, 3(1), 39-47. (Both researchers work in the

neuropharmacological research unit of the University of Karachi Biochemistry

Department.)

I could not gain access to the full article, but I could access the abstract. This study focused

on Escitalopram, an SSRI that is significant in its near-exclusivity for serotonin transporters.

When administered to mice, the subjects were found to be more exploratory in confined

experimental conditions, but showed a decreased willingness to explore in open field conditions,

perhaps indicating an increased confidence, but higher awareness for danger.

 4. Duric, V., Banasr, M., Franklin, T., Lepack, A., Adham, N., Kiss, B., Gyertyan, I., &

Duman, R.S. (2017). Cariprazine exhibits anxiolytic and dopamine D3 receptor-

dependent antidepressant effects in the chronic stress model. International Journal of

Neuropsychopharmacology, 20(10), 788-96. (The researchers hailed from all over the

world, including Yale University, Des Moines University, Toronto’s Campbell Family

Mental Health Research Institute, and multiple Hungarian institutes and universities. All

pertained to pharmacology and/or psychiatry.)

Much like the previous article, this study was performed to study the anxiolytic,

antidepressant, and stress-relieving effects of the dopamine receptor agonist cariprazine, mostly

prescribed as an antipsychotic. The drug was found to perform in a similar capacity to another

antipsychotic aripiprazole but is unique in its extremely high affinity for dopamine-3 receptors

(higher than even dopamine). It is suggested that this affinity is responsible for the antidepressant

and anxiolytic effects, although the specific mechanism is not well understood at this time.

5. Pelgrim, C.E., Peterson, J.D., Gosker, H.R., Schols, A.M.W.J., van Helvoort, A., Garssen,

J., Folkerts, G., & Kraneveld, A.D. (2019). Psychological co-morbidities in COPD:

Targeting systemic inflammation, a benefit for both? European Journal of

Pharmacology, 842, 99-110. (Researchers were all from either Utrecht University or

Maastricht University in the Netherlands and focused on pharmacology, nutrition, and

immunology.)
 This article focused on the disease chronic obstructive pulmonary disease (COPD), the fourth

most common cause of death in the world and the psychological effects of having the disease,

including anxiety and mental impairment (most likely due to decreased oxygen to the brain). It

analyzed current treatments for both COPD and its associated mental diseases and proposed

multiple new approaches to treating the mental comorbidities through anti-inflammation; the

obvious anti-inflammatory drugs such as phosphodiesterase-4 inhibitors were suggested, as well

as dietary supplements such as omega-3, anti-oxidants, or prebiotics that enhance brain

performance. The article also called for enhanced treatment of mental disorders in COPD

patients as less than a third of co-diagnosed patients are actively being treated for their anxiety

and/or depression.