Article
Chemistry, Multidisciplinary
Alexander M. Sherwood, Elise K. Burkhartzmeyer, Samuel E. Williamson, Michael T. Faley
Summary: A two-step divergent process was used to synthesize optically pure enantiomers of MDMA and MDA, which are clinically relevant phenylisopropylamine entactogens, from commercially available alanine-derived aziridines. Critical process parameters were identified and optimized to achieve gram-scale isolations without the need for chromatographic purification. The target compounds, (R)-(-)-MDMA, (S)-(+)-MDMA, (R)-(-)-MDA, and (S)-(+)-MDA, were obtained with purity greater than 98% by UPLC, enantiomeric excess greater than 99%, and net yields between 50 and 60% for the complete process.
Article
Biology
Richard McFarland, S. Peter Henzi, Andrea Fuller, Robyn S. Hetem, Christopher Young, Louise Barrett
Summary: Most primates, including humans, give birth during the inactive phase of the daily cycle. However, our understanding of the timing of nocturnal birth in wild diurnal primates is limited. This study measured maternal core body temperature during 24 births in wild vervet monkeys and found distinct changes in temperature during the birth process. Vervet monkeys typically give birth during their inactive phase, in sync with the lowest point of the maternal daily temperature rhythm, but individual variations in temperature during birth were observed. These findings suggest that the timing of primate birth may be influenced by the lower night-time temperatures and improve thermal efficiency during birth.
Article
Biochemistry & Molecular Biology
Mikhail Krasavin, Alexey Lukin, Ilya Sukhanov, Andrey S. Gerasimov, Savelii Kuvarzin, Evgeniya V. Efimova, Mariia Dorofeikova, Anna Nichugovskaya, Andrey Matveev, Kirill Onokhin, Konstantin Zakharov, Maxim Gureev, Raul R. Gainetdinov
Summary: This study screened an in-house library of compounds for agonistic activity towards TAAR1, resulting in the discovery of a potent TAAR1 agonist. Further in vivo tests demonstrated its efficacy in schizophrenia-related experiments. More preclinical studies are needed to evaluate its potential as a pharmacotherapy option for schizophrenia and other psychiatric disorders.
Article
Materials Science, Multidisciplinary
L. Prodan, I. Filippova, A. O. Zubtsovskii, S. Shova, S. Widmann, A. A. Tsirlin, I. Kezsmarki, V. Tsurkan
Summary: We investigate the crystal structure, magnetization, and specific heat measurements of single crystals of the hexagonal polar magnet Co2-xZnxMo3O8. It is found that Zn doping can preserve the robust antiferromagnetic behavior in Co2Mo3O8 up to x = 0.55. The observed effects in the lattice parameter, Curie-Weiss temperature, and magnetic entropy can be attributed to the site-selective Zn substitution, which is dependent on the coordination of the Co2+ ions.
Article
Medicine, Research & Experimental
Varsha Ananthapadmanabhan, Thomas C. Frost, Kara M. Soroko, Aine Knott, Brianna J. Magliozzi, Prafulla C. Gokhale, Vijaya G. Tirunagaru, Robert C. Doebele, James A. DeCaprio
Summary: In this study, the efficacy of milademetan, an MDM2 inhibitor, was assessed in various MCC models, showing significant inhibition on WT p53 MCC tumors. Useful in vitro and in vivo models for future MCC studies were also reported.
Article
Pharmacology & Pharmacy
Ulrich Gergs, Tobias Brueckner, Britt Hofmann, Joachim Neumann
Summary: The study revealed that lowering temperature can increase arrhythmias in mice overexpressing the human 5-HT4 receptor in their cardiac myocytes, suggesting a potential link between 5-HT4 receptors and hypothermia-induced arrhythmias in human patients.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Benjamin E. Blass, Peng-Jen Chen, John C. Gordon
Summary: Cocaine use disorder is a significant medical need without approved pharmacotherapies. The D3 dopamine receptor is a potential therapeutic target under investigation for addressing this issue.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Chemistry, Medicinal
Maali D. Alshammari, Pavel V. Kucheryavy, Nicole M. Ashpole, David A. Colby
Summary: The synthesis of flavones with fluorine substitutions has been reported, and their biological evaluation showed enhanced antioxidant activity and conserved neuroprotective activity compared to their non-fluorinated counterparts. Additionally, 3-fluoro-3',4',5'-trihydroxyflavone can serve as an NMR probe to detect structural changes during its action as a radical scavenger.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Organic
Arun K. Ghosh, Monika Yadav
Summary: The study focused on the base mediated asymmetric intramolecular oxidopyrylium-alkene [5 + 2]-cycloaddition reaction to synthesize functionalized tricyclic ring systems with an 8-oxabicyclo[3.2.1]octane core. The intramolecular cycloaddition resulted in the construction of two new rings, three new stereogenic centers, and high diastereoselectivity in the isolated yield. The size of alkyl groups and alkene tether length were found to affect the diastereoselectivity of the cycloadduct.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Spectroscopy
Yesim S. Kara, Mustafa Unsal, Nalan Tekin, Asli Esme
Summary: In this study, two novel oxadiazole derivatives were synthesized and their relationship with solvent effects was investigated using experimental and theoretical analyses. The linear solvation energy relationships showed better correlation with the vibrational frequencies of the compounds than other empirical solvent parameters. Additionally, the quadratic equation provided more accurate predictions for the vibrational frequency locations compared to the Swain and linear solvation energy relationships equations.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2021)
Article
Psychiatry
Adam Wysokinski, Elzbieta Kozlowska, Ewa Szczepocka, Anna Lucka, Justyna Agier, Ewa Brzezinska-Blaszczyk, Katarzyna Sobierajska
Summary: Schizophrenia patients exhibit a distinctive mRNA expression profile of dopamine and serotonin receptors in peripheral blood mononuclear cells. This expression is minimally affected by antipsychotic treatment, suggesting it may serve as a useful diagnostic biomarker for schizophrenia.
FRONTIERS IN PSYCHIATRY
(2021)
Article
Biochemistry & Molecular Biology
Chintha Venkataramaiah, Bandila Lakshmi Priya, Wudayagiri Rajendra
Summary: The study found that a bioactive compound isolated from Celastrus paniculatus has neuroprotective potential against ketamine-induced schizophrenia by modulating the CNS monoamine neurotransmitter system and alleviating neurological dysfunction associated with monoaminergic abnormalities.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Physics, Applied
Sambunath Das, Dayasindhu Dey, S. Ramasesha, Manoranjan Kumar
Summary: The study investigates quantum phase transitions of frustrated antiferromagnetic Heisenberg spin-1 systems on skewed two leg ladder geometries. The ground state switches from singlet to magnetic state with the variation of parameters, and can exhibit spiral spin arrangements. The switching pattern is nonmonotonic and dependent on system size, with specific parameter values leading to degeneracy and symmetry breaking.
JOURNAL OF APPLIED PHYSICS
(2021)
Article
Chemistry, Multidisciplinary
Jun Yang, Pan Zhang, Zeyuan Shen, Zhi-Xiang Yu
Summary: A Rh-catalyzed [4+3]/[4+1] cycloaddition reaction was reported, allowing the synthesis of compounds with a 5/7/5 tricyclic skeleton found in natural products. The scope of the reaction was investigated, as well as the further transformation of the cycloadduct. Computational studies were carried out to understand the mechanism of the [4+3]/[4+1] reaction and why the competing [4+3] reaction is disfavored.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Nursing
Tara Wood, Margret Johnson, Taryn Temples, Curry Bordelon
Summary: Thermoregulation is vital for the stability and long-term outcomes of newborns and critically-ill neonates. Maintaining a thermoneutral environment helps enhance growth, decrease respiratory support, reduce oxygen requirements, stabilize glucose levels, and reduce mortality and morbidities associated with abnormal thermal control. Heat exchange occurs through evaporation, conduction, convection, and radiation, and recognizing the methods of heat loss or gain is crucial in supporting a thermoneutral neonatal environment.
Editorial Material
Pharmacology & Pharmacy
Michael J. Curtis, Steve Alexander, Giuseppe Cirino, James R. Docherty, Christopher H. George, Mark A. Giembycz, Daniel Hoyer, Paul A. Insel, Angelo A. Izzo, Yong Ji, David J. MacEwan, Christopher G. Sobey, S. Clare Stanford, Mauro M. Teixeira, Sue Wonnacott, Amrita Ahluwalia
BRITISH JOURNAL OF PHARMACOLOGY
(2018)
Article
Gastroenterology & Hepatology
P. Aiden McCormick, Dermot E. Malone, James R. Docherty, Clifford Kiat, Brian T. Christopher, Jun Liong Chin
EUROPEAN JOURNAL OF GASTROENTEROLOGY & HEPATOLOGY
(2019)
Article
Pharmacology & Pharmacy
Hadeel A. Alsufyani, James R. Docherty
EUROPEAN JOURNAL OF PHARMACOLOGY
(2019)
Review
Pharmacology & Pharmacy
James R. Docherty
EUROPEAN JOURNAL OF PHARMACOLOGY
(2019)
Article
Gastroenterology & Hepatology
Peter Aiden McCormick, James R. Docherty
EUROPEAN JOURNAL OF GASTROENTEROLOGY & HEPATOLOGY
(2020)
Editorial Material
Pharmacology & Pharmacy
Christopher H. George, Stephen P. H. Alexander, Giuseppe Cirino, James R. Docherty, Daniel Hoyer, Paul A. Insel, Angelo A. Izzo, Yong Ji, Reynold A. Panettieri, Christopher G. Sobey, S. Clare Stanford, Barbara Stefanska, Gary Stephens, Mauro Teixeira, Amrita Ahluwalia
BRITISH JOURNAL OF PHARMACOLOGY
(2019)
Editorial Material
Pharmacology & Pharmacy
Angelo A. Izzo, Mauro Teixeira, Steve P. H. Alexander, Giuseppe Cirino, James R. Docherty, Christopher H. George, Paul A. Insel, Yong Ji, David A. Kendall, Reynold A. Panattieri, Christopher G. Sobey, S. Clare Stanford, Barbara Stefanska, Gary Stephens, Amrita Ahluwalia
BRITISH JOURNAL OF PHARMACOLOGY
(2020)
Article
Biochemistry & Molecular Biology
Reece G. Kenny, Ziga Ude, James R. Docherty, Celine J. Marmion
JOURNAL OF INORGANIC BIOCHEMISTRY
(2020)
Review
Pharmacology & Pharmacy
Hadeel A. Alsufyani, James R. Docherty
SAUDI PHARMACEUTICAL JOURNAL
(2020)
Article
Pharmacology & Pharmacy
Hadeel A. Alsufyani, James R. Docherty
Summary: The rat portal vein exhibits phasic and tonic contractions in response to the alpha(1)-adrenoceptor agonist phenylephrine, which are mediated by different subtypes of alpha(1)-adrenoceptors. The effects of prazosin and RS100329 on phenylephrine potency differ significantly, while fasudil primarily affects tonic contractions.
CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Hadeel A. Alsufyani, P. Aiden McCormick, James R. Docherty
Summary: The contraction of rat spleen to adrenergic agonists involves alpha(2)- and alpha(1B)-adrenoceptors, with a lesser role for alpha(1A)-adrenoceptors. This confirms the suggestion that smooth muscle contractions commonly involve multiple subtypes.
PHARMACOLOGICAL REPORTS
(2021)
Review
Pharmacology & Pharmacy
James R. Docherty, Hadeel A. Alsufyani
Summary: The majority of illicit stimulants act on monoaminergic systems, causing both stimulant effects and adverse reactions. These substances can interact with monoamine transporters and receptors, as well as mimicking monoamine actions. Stimulants, particularly MDMA, can increase the risk of sudden cardiac death and fatalities from hyperthermia, especially in hot conditions like raves. This review focuses on the pharmacology of cardiovascular and temperature adverse effects of stimulants.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
James R. Docherty, Hadeel A. Alsufyani
Summary: The effects of psychostimulants involve various neurotransmitter pathways and can lead to serious adverse events, including potentially life-threatening hyperthermia. Recreational users should be aware of the dangers associated with these substances.
JOURNAL OF CLINICAL PHARMACOLOGY
(2021)
Review
Obstetrics & Gynecology
P. A. McCormick, M. Higgins, C. A. McCormick, N. Nolan, J. R. Docherty
Summary: HELLP syndrome is a rare pregnancy-related condition characterized by hemolysis, elevated liver function tests, and low platelets. The main driver is suggested to be vasospasm, leading to hepatic ischemia, infarction, and hemorrhage. Besides hepatic complications, other issues like placental abruption, acute renal failure, and posterior reversible encephalopathy syndrome may also be linked to regional vasospasm.
JOURNAL OF MATERNAL-FETAL & NEONATAL MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Hadeel A. Alsufyani, James R. Docherty
Summary: This study examined the roles of alpha(1)-adrenoceptors and purinoceptors in contractions of the mouse vas deferens in response to different frequencies of stimulation. The results suggest that a combination of non-selective alpha(1)-adrenoceptor blockade, particularly alpha(1)(B)-adrenoceptor blockade, along with P2X1 purinoceptor blockade, is useful in reducing male fertility.
KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY
(2021)