A mediastinum-tumour-like pulmonary arteriovenous malformation with association to the pulmonary artery treated with surgical resection.

Despite embolization being now considered the preferred treatment for PAVM, surgical intervention may be considered if the malformation involves large vessels.

Characteristics of patients in inpatient psychiatry during the COVID-19 pandemic.

To date, there have been limited publications examining the characteristics of psychiatric patients with COVID-19 in an inpatient setting. In this retrospective cohort review, we attempted to categorize the differences between patients admitted to the COVID unit versus the non-COVID unit using data from a community hospital located on Long Island, NY. We found that patients admitted to the COVID-19 unit had on average longer lengths of stay, were more likely to belong to non-white racial groups, and were less likely to be smokers.

4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1.

Herein, we report the identification, design, and synthesis of a series of 4-substituted 2-amino-3,4-dihydroquinazolines with hairpin turn side chains as novel inhibitors of BACE-1. The dihydroquinazoline derivatives were rationally designed by modifying the amide group and relocating the α -hydrophobic substituent on the hairpin turn side chain of lead compound 2 to the C4-position on the 3,4-dihydroquinazoline scaffold to facilitate interactions with the S1, S2 and S1' subsites of BACE-1. Among these derivatives, two compounds exhibited potent BACE-1 inhibitory activity: 4-methyl-substituted (22a, BACE-1 CFA IC50 = 0.38 µM; BACE-1 WCA IC50 = 0.14 µM) and 4-cyclohexylmethyl-substituted (22b, BACE-1 CFA IC50 = 0.49 µM; BACE-1 WCA IC50 = 0.14 µM) 2-amino-3,4-dihydroquinazoline, each bearing a side chain of N-cyclohexyl-N-((1-methyl-1H-pyrazol-4-yl)methyl amide. The results suggest that the structural modifications maintain the hairpin turn topology similar to that of compound 2 and provide an additional interaction with the S2 subsite.

Synthetic cannabinoid use among college students.

BACKGROUND AND OBJECTIVES: Synthetic cannabinoid use is associated with severe problems, including psychosis, kidney failure, and death. Given that young adults are especially vulnerable to using synthetic cannabinoids, the current study sought to identify factors and consequences related to use within this population. METHODS: 1140 undergraduates completed an online survey of synthetic cannabinoid use, consequences, and related constructs. RESULTS: The prevalence of lifetime synthetic cannabinoid use was 7.9% (n = 90), 15.6% (n = 13) of which were regular users, meaning they used once a year or more often. Synthetic cannabinoid users reported multiple adverse effects (e.g., anxiety, paranoia, tachycardia, lightheadedness) and 16.7% (n = 15) of users said they considered or did go to the Emergency Room while using synthetic cannabinoids. In the entire sample, participants believed their friends (t = 18.3, p < .001) and students in general (t = 46.0, p < .001) use synthetic cannabinoids more than they do. Natural cannabis users were associated with increased odds of having tried synthetic cannabinoids than those who had never used natural cannabis, OR = 7.63 (4.44 to 13.14) p < .0001, and 92.2% (n = 83) of synthetic cannabinoid users reported lifetime use of natural cannabis. Common reasons for use were legality, not appearing on drug tests, and availability, not that students enjoyed using synthetic cannabinoids or thought they were safe to use. DISCUSSION AND CONCLUSIONS: Synthetic cannabinoid use is associated with a variety of negative consequences. The data also supports a strong link between natural cannabis use and synthetic cannabinoid use. SCIENTIFIC SIGNIFICANCE: Natural cannabis users appear to be a high-risk group for using synthetic cannabinoids. There are multiple negative effects associated with synthetic cannabinoid use and reasons for use relate to convenience vs. enjoyment. Data have important implications for prevention and treatment efforts.

Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors.

We demonstrate that the acrylamide group can be used to improve the drug-like properties of potential drug candidates. In the EGFR inhibitor development, both the solubility and membrane permeability properties of compounds 6a and 7, each containing an acrylamide group, were substantially better than those of gefitinib (1) and AZD3759 (2), respectively. We demonstrated that incorporation of an acrylamide moiety could serve as a good strategy for improving drug-like properties.

Dextromethorphan Addiction Mediated Through the NMDA System: Common Pathways With Alcohol?

Dextromethorphan, an antitussive (cough suppressant) drug of the morphinan class with sedative and dissociative properties found in cough syrup and other over-the-counter products, is also a substance of abuse, seen primarily in young adults all over the world. A case of dextromethorphan use disorder is presented in a 45-year-old women. Her repeated attempts at abstinence were unsuccessful secondary to continued intense cravings. Treatment with topiramate resulted in complete resolution of her cravings. Topiramate was chosen empirically because of a common action with dextromethorphan in the NMDA system. Genetic testing was obtained and the patient was found to be a carrier of the GRIK1 rs2832407(C:C) allele. The (C:C) allele has been associated with an increased risk of alcohol use disorder and a treatment response of patients with heavy drinking to topiramate. This case provides an opportunity to discuss personalized medicine (treatment options aided by the use of genetic testing) and the possible shared genetic susceptibility for dependence in 2 substances of abuse.