Article
Biochemistry & Molecular Biology
Hikaru Koizumi, Taichi Hiraga, Leandro K. Oharomari, Toshiaki Hata, Takeru Shima, Jang Soo Yook, Masahiro Okamoto, Akihiro Mouri, Toshitaka Nabeshima, Hideaki Soya
Summary: Schizophrenia may be attributed to perinatal neurodevelopmental deficits and influenced by environmental factors. Hypofrontality and dysfunction in glutamatergic and dopaminergic neurons are known factors, while early enriched environment and low-intensity exercise training during adolescence may help prevent and ameliorate the disease.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Review
Clinical Neurology
Anastasia Levinta, Shakila Meshkat, Roger S. McIntyre, Cameron Ho, Leanna M. W. Lui, Yena Lee, Rodrigo B. Mansur, Kayla M. Teopiz, Nelson B. Rodrigues, Joshua D. Di Vincenzo, Felicia Ceban, Joshua D. Rosenblat
Summary: Ketamine has demonstrated antidepressant efficacy in patients with treatment-resistant depression, although its effectiveness may be affected by the level of treatment resistance.
JOURNAL OF AFFECTIVE DISORDERS
(2022)
Review
Psychiatry
Shakila Meshkat, Joshua D. Rosenblat, Roger C. Ho, Taeho Greg Rhee, Bing Cao, Felicia Ceban, Kevork Danayan, Noah Chisamore, Joshua D. Di Vincenzo, Roger S. McIntyre
Summary: Ketamine may be effective in treating pediatric depression, but there are limitations in the current research, and larger-scale studies with different administration modalities are needed.
PSYCHIATRY RESEARCH
(2022)
Article
Medicine, Research & Experimental
Chintha Venkataramaiah, Sholapuri Payani, Bandila Lakshmi Priya, Jangampalli Adi Pradeepkiran
Summary: The glutamate and dopamine hypotheses are leading theories in the pathophysiology of schizophrenia, and new neuroprotective compounds from medicinal plants could offer benefits. A novel bioactive compound found in Celastrus paniculatus shows potential neuroprotective effects in ketamine-induced schizophrenia, particularly in regulating glutamate metabolism.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Review
Pharmacology & Pharmacy
Karolina Podkowa, Kamil Czarnacki, Agnieszka Boronczyk, Michal Boronczyk, Justyna Paprocka
Summary: Migraine, a disorder that affects females more often than males, may be treated with NMDA receptor antagonists such as memantine and ketamine, according to a comprehensive literature review. Animal and in vitro studies have shown that these drugs inhibit the propagation of spreading depression (SD), a major mechanism in migraine pathophysiology. Clinical trials have also indicated that ketamine or memantine may be effective in treating severe migraine, although more studies with control groups are needed. These drugs could be a promising alternative for individuals with treatment-resistant migraine with aura or limited treatment options.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2023)
Article
Behavioral Sciences
Bethany H. Dennis, Stuart A. Neale, Fiona E. N. LeBeau, Thomas E. Salt
Summary: Aberrant cortical oscillations in the beta and gamma range are associated with symptoms of schizophrenia and other psychiatric conditions. Activation of Group II mGlu receptors, and mGlu2 specifically, with orthosteric agonists reduced the power of both beta and gamma oscillations in ACC without a significant effect on oscillation peak frequencies.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2023)
Review
Psychiatry
Jiaqi Xiong, Orly Lipsitz, David Chen-Li, Joshua D. Rosenblat, Nelson B. Rodrigues, Isabelle Carvalho, Leanna M. W. Lui, Hartej Gill, Flora Narsi, Rodrigo B. Mansur, Yena Lee, Roger S. McIntyre
Summary: The study aimed to evaluate the acute anti-suicidal ideation effects of single-dose ketamine in different formulations and routes of administration by pooling the results from randomized controlled trials. The findings suggest that intravenous ketamine and intranasal esketamine are associated with robust reductions in suicidal thoughts at 2-h, 4-h, and 24-h post-intervention. Further research on intramuscular, oral, and sublingual ketamine, as well as comparative studies, are needed to evaluate the efficacy of these formulations and routes of administration in reducing suicidal ideation.
JOURNAL OF PSYCHIATRIC RESEARCH
(2021)
Article
Psychiatry
Orly Lipsitz, Roger S. McIntyre, Nelson B. Rodrigues, Yena Lee, Danielle S. Cha, Hartej Gill, Mehala Subramaniapillai, Kevin Kratiuk, Kangguang Lin, Roger Ho, Rodrigo B. Mansur, Joshua D. Rosenblat
Summary: The study found that menopausal status does not influence the overall treatment response of women with TRD receiving IV ketamine. Both premenopausal and postmenopausal participants showed similar response rates and remission rates to IV ketamine treatment following four infusions, but premenopausal women experienced improvements in social function more rapidly, while postmenopausal women experienced reduction in suicidal ideation more rapidly.
JOURNAL OF PSYCHIATRIC RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Samantha V. Abram, Brian J. Roach, Susanna L. Fryer, Vince D. Calhoun, Adrian Preda, Theo G. M. van Erp, Juan R. Bustillo, Kelvin O. Lim, Rachel L. Loewy, Barbara K. Stuart, John H. Krystal, Judith M. Ford, Daniel H. Mathalon
Summary: NMDAR hypofunction is a leading pathophysiological model of schizophrenia. Resting-state functional magnetic resonance imaging (rsfMRI) studies demonstrate thalamic dysconnectivity pattern in schizophrenia involving excessive connectivity with sensory regions and deficient connectivity with frontal, cerebellar, and thalamic regions. Ketamine, an NMDAR antagonist, induces schizophrenia-like symptoms and alters rsfMRI thalamic connectivity. This study confirms that ketamine-induced thalamic dysconnectivity resembles the thalamic dysconnectivity observed in schizophrenia, which suggests the contribution of NMDAR hypofunction to the pathophysiology of schizophrenia.
MOLECULAR PSYCHIATRY
(2022)
Article
Clinical Neurology
Orly Lipsitz, Roger S. McIntyre, Nelson B. Rodrigues, Tyler S. Kaster, Danielle S. Cha, Elisa Brietzke, Hartej Gill, Flora Nasri, Kangguang Lin, Mehala Subramaniapillai, Kevin Kratiuk, Kayla Teopiz, Leanna M. W. Lui, Yena Lee, Roger Ho, Margarita Shekotikhina, Rodrigo B. Mansur, Joshua D. Rosenblat
Summary: Early improvement with IV ketamine treatment predicts treatment response in depression patients. Even without early improvements, patients may still experience significant symptom reduction after four infusions.
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
(2021)
Review
Pharmacology & Pharmacy
Lily R. Aleksandrova, Anthony G. Phillips
Summary: The emerging therapeutic efficacy of ketamine and classical psychedelics for depression has sparked considerable interest in the mechanisms underlying neuroplasticity. Preclinical and clinical evidence suggests that these drugs induce synaptic, structural, and functional changes, particularly in pyramidal neurons in the prefrontal cortex, resulting in adaptive rewiring of pathological neurocircuitry.
TRENDS IN PHARMACOLOGICAL SCIENCES
(2021)
Article
Neurosciences
Amit Kumar, Ansab Akhtar, Anurag Kuhad, Sangeeta Pilkhwal Sah
Summary: This study found that sarcosine can alleviate the behavioral symptoms of schizophrenia by modulating oxidative stress, neuroinflammation, and mitochondrial dysfunction.
EXPERIMENTAL BRAIN RESEARCH
(2023)
Review
Psychology, Clinical
Tharcila V. Chaves, Bob Wilffert, Zila M. Sanchez
Summary: This review aims to outline the cases of overdose and death related to the use of ketamine and/or its analogues and investigating the safety of ketamine as an antidepressant in a therapeutic context. The results of the study showed that the misuse of ketamine and/or its analogues can lead to fatal consequences, but no cases of overdose or death were found in the therapeutic use of ketamine as an antidepressant.
AMERICAN JOURNAL OF DRUG AND ALCOHOL ABUSE
(2023)
Article
Chemistry, Medicinal
Comfort A. Boateng, Ashley N. Nilson, Rebekah Placide, Mimi L. Pham, Franziska M. Jakobs, Noelia Boldizsar, Scot Mcintosh, Leia S. Stallings, Ivana V. Korankyi, Shreya Kelshikar, Nisha Shah, Diandra Panasis, Abigail Muccilli, Maria Ladik, Brianna Maslonka, Connor McBride, Moises Ximello Sanchez, Ebrar Akca, Mohammad Alkhatib, Julianna Saez, Catherine Nguyen, Emily Kurtyan, Jacquelyn DePierro, Raymond Crowthers, Dylan Brunt, Alessandro Bonifazi, Amy Hauck Newman, Rana Rais, Barbara S. Slusher, R. Benjamin Free, David R. Sibley, Kent D. Stewart, Chun Wu, Scott E. Hemby, Thomas M. Keck
Summary: This study focuses on the pharmacological targeting of dopamine D-4 receptor (D4R) for the treatment of neuropsychiatric disorders. A series of benzothiazole analogues with high D4R binding affinity and selectivity were synthesized and evaluated. One of the novel analogues, 16f, showed promising results as a low-efficacy D4R partial agonist, with metabolic stability and good brain penetration in rats. It also decreased cocaine self-administration in a dose-dependent manner, supporting further efforts to target D4R in substance use disorder (SUD) treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Jin Cai, Mingqi Huang, Yuhong Wang, Xixi Chen, Min Ji
Summary: Three series of novel bitopic benzopyranomorpholine analogues were designed, synthesized, and evaluated for their selective ligand activity for the dopamine D3 receptor. Most compounds showed strong binding affinities and selectivity for the D3 receptor. One compound, 20h, demonstrated nanomolar affinity for the D3 receptor and exhibited anti-drug addiction efficacy in animal models.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Applied
Jiang-Er Lan, Xiao-Jin Li, Xiao-Feng Zhu, Zhong-Lin Sun, Jian-Ming He, Mire Zloh, Simon Gibbons, Qing Mu
Summary: This study identified five flavonoids from the traditional Chinese herb Artemisia rupestris L., which showed synergistic antibacterial effects against multidrug-resistant Staphylococcus aureus. Three of the compounds exhibited synergy when combined with norfloxacin against fluoroquinolone-resistant strains, and further investigations were conducted to explore the mechanisms of the synergistic effects.
NATURAL PRODUCT RESEARCH
(2021)
Article
Biology
Nilkanth Patel, Xi Ping Huang, Jessica M. Grandner, Linda C. Johansson, Benjamin Stauch, John D. McCorvy, Yongfeng Liu, Bryan Roth, Vsevolod Katritch
Article
Plant Sciences
Gugu F. Sibandze, Paul Stapleton, Simon Gibbons
JOURNAL OF NATURAL PRODUCTS
(2020)
Article
Integrative & Complementary Medicine
Awo Afi Kwapong, Sarah Soares, Stephen Ping Teo, Paul Stapleton, Simon Gibbons
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2020)
Article
Infectious Diseases
Zhong-Lin Sun, Shi-Chang Sun, Jian-Ming He, Jiang-Er Lan, Simon Gibbons, Qing Mu
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
(2020)
Article
Biochemistry & Molecular Biology
Aljawharah AlQathama, Luying Shao, Ammar Bader, Proma Khondkar, Simon Gibbons, Jose M. Prieto
Article
Biochemistry & Molecular Biology
Xi-Ping Huang, Terrence P. Kenakin, Shuo Gu, Brian K. Shoichet, Bryan L. Roth
Article
Clinical Neurology
Allison N. White, Joshua D. Gross, Shane W. Kaski, Kristen R. Trexler, Kim A. Wixi, Wittiam C. Wetsel, Steven G. Kinsey, David P. Siderovski, Vincent Setola
JOURNAL OF PSYCHOPHARMACOLOGY
(2020)
Article
Chemistry, Organic
Chuan-Yun Xiao, Zhong-Lin Sun, Jiao Huang, Rong-Sheng Li, Jian-Ming He, Simon Gibbons, Dian-Wen Ju, Qing Mu
Summary: This study identified 10 new neolignans from the extract of Piper betle leaves and confirmed their synergistic antibacterial activity with norfloxacin against a drug-resistant strain of Staphylococcus aureus. Computational molecular modeling also suggested the binding of certain compounds to the active site of the NorA efflux pump.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Infectious Diseases
Stephen P. Teo, Sanjib Bhakta, Paul Stapleton, Simon Gibbons
Article
Biochemistry & Molecular Biology
Peiyu Xu, Sijie Huang, Chunyou Mao, Brian E. Krumm, X. Edward Zhou, Yangxia Tan, Xi-Ping Huang, Yongfeng Liu, Dan-Dan Shen, Yi Jiang, Xuekui Yu, Hualiang Jiang, Karsten Melcher, Bryan L. Roth, Xi Cheng, Yan Zhang, H. Eric Xu
Summary: The study reported two cryo-EM structures of human D3R in complex with an inhibitory G protein and bound to D3R-selective agonists PD128907 and pramipexole, revealing distinct agonist binding modes and conformational signatures for ligand-induced receptor activation, providing insights for designing specific ligands to treat CNS diseases targeting the dopaminergic system.
Review
Biotechnology & Applied Microbiology
Atanas G. Atanasov, Sergey B. Zotchev, Verena M. Dirsch, Claudiu T. Supuran
Summary: Natural products and their analogues have historically played a significant role in pharmacotherapy, however, they also present challenges. Recent technological and scientific developments are addressing these challenges and revitalizing interest in natural products as drug leads, particularly for combating antimicrobial resistance.
NATURE REVIEWS DRUG DISCOVERY
(2021)
Editorial Material
Plant Sciences
Marcy J. Balunas, Gordon M. Cragg, Simon Gibbons, Rachel Mata
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Infectious Diseases
Cynthia Amaning Danquah, Michael Tetteh, Isaac Kingsley Amponsah, Abraham Yeboah Mensah, Kwame Ohene Buabeng, Simon Gibbons, Sanjib Bhakta
Summary: This study found that bulb extracts of Ghanaian shallots exhibited inhibitory effects on Mycobacterium smegmatis and Escherichia coli, as well as efflux pump and biofilm inhibitory activities against various bacterial strains. The results suggest that Ghanaian shallots could be potentially valuable in combating antimicrobial resistance, especially in tuberculosis.
Article
Multidisciplinary Sciences
Joshua Pottel, Duncan Armstrong, Ling Zou, Alexander Fekete, Xi-Ping Huang, Hayarpi Torosyan, Dallas Bednarczyk, Steven Whitebread, Barun Bhhatarai, Guiqing Liang, Hong Jin, S. Nassir Ghaemi, Samuel Slocum, Katalin V. Lukacs, John J. Irwin, Ellen L. Berg, Kathleen M. Giacomini, Bryan L. Roth, Brian K. Shoichet, Laszlo Urban
