Article
Chemistry, Medicinal
Andhika B. B. Mahardhika, Anastasiia Ressemann, Sarah E. E. Kremers, Mariana S. Gregorio S. Castanheira, Clara T. T. Schoeder, Christa E. E. Mueller, Thanigaimalai Pillaiyar
Summary: The study synthesized a series of DIM derivatives and evaluated their affinities and efficacies for human CB receptor subtypes. The compound di-(4-cyano-1H-indol-3-yl)methane showed the highest potency as a CB2 receptor agonist and has potential as a novel drug for inflammatory diseases.
ARCHIV DER PHARMAZIE
(2023)
Review
Neurosciences
Mengya Wang, Huayuan Liu, Zegang Ma
Summary: Parkinson's disease is a neurodegenerative disease influenced by the cannabinoid system in the basal ganglia. Modulating the endogenous cannabinoid levels can have an anti-movement disorder effect, suggesting the development of drugs targeting the cannabinoid system as a novel strategy for Parkinson's disease treatment.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2022)
Article
Chemistry, Medicinal
Toni Kline, Cong Xu, Faith R. Kreitzer, Dow P. Hurst, Khalil M. Eldeeb, Jim Wager-Miller, Kathleen Olivas, Seon A. Hepburn, John W. Huffman, Ken Mackie, Allyn C. Howlett, Patricia Reggio, Nephi Stella
Summary: The author synthesized fourteen novel alkylindole analogues and evaluated their activities at alkylindole-sensitive GPCRs. They found three characteristics that favor binding to alkylindole-sensitive GPCRs versus CB1R/CB2R and identified novel chemical tools for studying alkylindole-sensitive GPCRs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Lukasz Zapala, Grzegorz Niemczyk, Piotr Zapala, Artur Wdowiak, Iwona Bojar, Tomasz Kluz, Aleksandra Szopa, Anna Serefko, Piotr Radziszewski, Andrzej Wrobel
Summary: This paper aimed to investigate whether the selective cannabinoid CB1 receptor agonist ACEA could reverse the effects of corticosterone (CORT) on depressive and overactive bladder potential. Through experiments on 48 female rats, it was found that ACEA could restore CORT-induced bladder dysfunction and depressive behavior, as well as regulate urine and other biomarkers.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Esty Goldberger, Merav Tauber, Yair Ben-Chaim
Summary: Cannabinoids produce their effects by binding to CB1 and CB2 receptors, and recent studies have shown that membrane potential may modulate the activity of the CB1 receptor. The voltage dependence appears to be agonist-specific, which could contribute to our understanding of the physiological functions mediated by the endocannabinoid system.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Almudena Robledo-Menendez, Maria Vella, Pedro Grandes, Edgar Soria-Gomez
Summary: Hippocampal circuits play a crucial role in cognitive performance and are deeply affected in pathological conditions. Cannabinoid receptors regulate different cell types within hippocampal circuitries. Understanding the precise mechanisms triggered by cannabinoid receptor activation at a cellular and subcellular level helps in grasping hippocampal pathophysiological states.
Article
Neurosciences
Grant C. Glatfelter, John S. Partilla, Michael H. Baumann
Summary: Synthetic cannabinoid receptor agonists (SCRAs) are a new class of psychoactive substances found on recreational drug markets worldwide. 5F-MDMB-PICA, a popular SCRA, is a potent agonist at CB1 receptors. In vitro and in vivo studies showed that subtle alterations to head group composition can have profound influence on pharmacological effects at CB1. The SCRA-induced effects in mice such as hypothermia, catalepsy, and analgesia were dose- and time-dependent and reversed by rimonabant, indicating CB1 involvement.
NEUROPSYCHOPHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Chris S. S. Breivogel, Bonnie M. M. Brenseke, Khalil Eldeeb, Katlyn Nichols, Amreen Jonas, Artik H. H. Mistry, Laura Barbalato, Nicholas Luibil, Allyn C. C. Howlett, Sandra Leone-Kabler, Rob P. H. Hilgers, Victor M. M. Pulgar
Summary: This study found that the AAI CB1 agonist JWH-073, found in K2/Spice brands, may cause greater vascular adverse events compared to Delta(9)-THC, the primary CB1 agonist found in cannabis.
CANNABIS AND CANNABINOID RESEARCH
(2023)
Article
Chemistry, Medicinal
Florian Mohr, Thomas Hurrle, Lindsey Burggraaff, Lukas Langer, Martijn P. Bemelmans, Maximilian Knab, Martin Nieger, Gerard J. P. van Westen, Laura H. Heitman, Stefan Braese
Summary: The study reports the development and evaluation of structure-activity relationship of a series of modified coumarins as cannabinoid receptor ligands. The most potent coumarins showed a CB2 selective agonistic profile with low nanomolar affinities, and several crucial structural requirements were identified through the research.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Leontina Elena Filipiuc, Daniela Carmen Ababei, Teodora Alexa-Stratulat, Cosmin Vasilica Pricope, Veronica Bild, Raluca Stefanescu, Gabriela Dumitrita Stanciu, Bogdan-Ionel Tamba
Summary: The discovery of the pharmacological effects of cannabis, traditionally used in Asia, has led to the development of new compounds for treating various diseases. Recent research suggests that these effects may not only involve cannabinoid receptors, but also other mechanisms yet to be fully understood.
Review
Plant Sciences
Henry Lowe, Blair Steele, Joseph Bryant, Ngeh Toyang, Wilfred Ngwa
Summary: This article discusses the potential medicinal value of non-cannabinoid compounds in the cannabis plant, such as flavonoids and terpenes, and highlights one promising non-cannabinoid molecule, Caflanone, for clinical trials. The article suggests that many phytochemicals in cannabis have wide therapeutic potential.
Review
Pharmacology & Pharmacy
Sofia M. Saraiva, Lucia Martin-Banderas, Matilde Duran-Lobato
Summary: The interest in using cannabinoids for medical applications, especially in treating eye conditions, has been growing. However, due to the unfavorable properties of cannabinoids and barriers for local administration in the eye, drug delivery systems are needed. This review focuses on identifying eye diseases that could be treated with cannabinoids, reviewing formulation properties, evaluating cannabinoid-based formulations for ocular administration, and exploring potential alternative formulations for eye administration.
Article
Clinical Neurology
Astrid Coronado-Alvarez, Karen Romero-Cordero, Lorena Macias-Triana, Agnes Tatum-Kuri, Alba Vera-Barron, Henning Budde, Sergio Machado, Tetsuya Yamamoto, Claudio Imperatori, Eric Murillo-Rodriguez
Summary: Δ9-THC, the major component of Cannabis sativa, exerts biological effects through activation of cannabinoid receptors CB1 and CB2. Synthetic CB1 cannabinoid receptor selective agonists show potential in therapeutic approaches, but concerns regarding side effects still exist despite positive results in experimental models and preclinical trials.
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
(2021)
Review
Plant Sciences
Chiara Maioli, Daiana Mattoteia, Hawraz Ibrahim M. Amin, Alberto Minassi, Diego Caprioglio
Summary: Cannabis is a significant source of bioactive natural products, and the minor cannabinoid CBN has important implications for global scientific research and the development of synthetic methodologies.
Article
Chemistry, Physical
Gabriele de Azevedo Cardoso, Ana Luiza de Andrade Querino, Heveline Silva, Joao Paulo Ataide Martins, Rossimiriam Pereira de Freitas, Rosemeire Brondi Alves
Summary: Twenty-two novel hybrid compounds of indolic cannabinoids and 1,2,3-triazoles were synthesized with high yields. These compounds showed antiproliferative activity against breast tumor cells, with 12 compounds exhibiting significant cytotoxicity. Derivative 18j and 18a were the most active compounds, with promising ADME parameters for further development as anticancer agents.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Toxicology
Richard C. Kevin, Alexander L. Kovach, Timothy W. Lefever, Thomas F. Gamage, Jenny L. Wiley, Iain S. McGregor, Brian F. Thomas
FORENSIC TOXICOLOGY
(2019)
Article
Pharmacology & Pharmacy
Thomas F. Gamage, Charlotte E. Farquhar, Ryan J. McKinnie, Richard C. Kevin, Lain S. McGregor, Mark L. Trudell, Jenny L. Wiley, Brian F. Thomas
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2019)
Article
Neurosciences
Jenny L. Wiley, Timothy W. Lefever, Michelle Glass, Brian F. Thomas
Article
Pharmacology & Pharmacy
Stevie C. Britch, Alan G. Goodman, Jenny L. Wiley, Abby M. Pondelick, Rebecca M. Craft
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2020)
Article
Behavioral Sciences
Thomas F. Gamage, Daniel G. Barrus, Richard C. Kevin, David B. Finlay, Timothy W. Lefever, Purvi R. Patel, Megan A. Grabenauer, Michelle Glass, Iain S. McGregor, Jenny L. Wiley, Brian F. Thomas
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2020)
Article
Clinical Neurology
Jenny L. Wiley, Daniel G. Barrus, Charlotte E. Farquhar, Timothy W. Lefever, Thomas F. Gamage
Summary: The study investigated the effects of age, sex, and rodent species on the psychoactive impact of intraperitoneal THC and its metabolite 11-OH-THC. The results show that 11-OH-THC exhibited higher potency in some aspects compared to THC, suggesting that species is a crucial design consideration in preclinical studies of phytocannabinoids.
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
(2021)
Article
Substance Abuse
L. Jenny Wiley, I. Shanequa Taylor, A. Julie Marusich
Summary: The study examined the effects of THC administered through different routes on rats. Results showed varying effects of THC across different routes of administration, providing empirical evidence for choosing the route of administration for mechanistic investigation of THC's pharmacology. Animal models using translationally relevant routes of administration may lead to more accurate predictions of THC effects in humans.
DRUG AND ALCOHOL DEPENDENCE
(2021)
Article
Chemistry, Analytical
Alexander L. Kovach, Randi R. Carter, Jonathan W. Thornburg, Robert Wiethe, Timothy R. Fennell, Jenny L. Wiley
Summary: Studies have found that vitamin E acetate undergoes thermal degradation in electronic vaping devices and is considered a major contributor to e-cigarette or vaping product use-associated lung injuries. By analyzing the degradation products of vitamin E acetate, researchers have identified two major compounds and suggested their potential as biomarkers for exposure and toxicity assessment.
JOURNAL OF ANALYTICAL TOXICOLOGY
(2022)
Article
Pharmacology & Pharmacy
David B. Finlay, Thuy Nguyen, Thomas F. Gamage, Shuli Chen, Daniel G. Barrus, Purvi R. Patel, Brian F. Thomas, Jenny L. Wiley, Yanan Zhang, Michelle Glass
Summary: This study compared the synthetic cannabinoid receptor agonist EG-018 and its analogues with existing putative neutral antagonists of CB1 receptor. The results showed highly variable signaling outcomes for EG-018 analogues, with some compounds demonstrating potential as neutral antagonists. These findings provide important insights for the development of CB1 neutral antagonists.
PHARMACOLOGY RESEARCH & PERSPECTIVES
(2022)
Article
Substance Abuse
S. O. Vanegas, A. M. Reck, C. E. Rodriguez, J. A. Marusich, O. Yassin, G. Sotzing, J. L. Wiley, S. G. Kinsey
Summary: This study evaluates the effects of acute and repeated exposure to delta(8)-THC and finds that it produces similar effects to delta(9)-THC, including risk of drug dependence and abuse liability.
DRUG AND ALCOHOL DEPENDENCE
(2022)
Article
Behavioral Sciences
Julie A. Marusich, Thomas F. Gamage, Yanan Zhang, Luli R. Akinfiresoye, Jenny L. Wiley
Summary: Synthetic cannabinoid receptor agonists (SCRAs) are a novel class of psychoactive substances that bind to and activate CB1 receptors in the brain.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2022)
Article
Behavioral Sciences
David B. Finlay, Warwick Mackie, Hunter D. J. Webb, Lucy R. Thomsen, Mhairi Nimick, Rhonda J. Rosengren, Julie A. Marusich, Michelle Glass, Jenny L. Wiley
Summary: AMB-FUBINACA is a synthetic cannabinoid receptor agonist associated with abuse and health harm. The study aimed to investigate the interactions between AMB-FUBINACA and pFPP in rats and mice. The results suggest that pFPP may attenuate some physiological effects of AMB-FUBINACA in rats, but there is little evidence of direct receptor interactions. Overall, combining pFPP and AMB-FUBINACA is unlikely to result in increased harm/toxicity.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2023)
Article
Cardiac & Cardiovascular Systems
Lucas T. Laudermilk, Julie A. Marusich, Jenny L. Wiley
Summary: This study investigates the effects of sex and route of administration on THC-induced changes in cardiopulmonary phenotypes in mice. The results demonstrate that THC alters respiratory minute volume and heart rate across different administration routes, with varying effects in duration and direction.
CARDIOVASCULAR TOXICOLOGY
(2023)
Article
Behavioral Sciences
Antony D. Abraham, Jenny L. Wiley, Julie A. Marusich
Summary: This study found that THC has an impact on nicotine intake in rat models, decreasing self-administration of nicotine and altering the dose-effect curve. Unlike nicotine, THC does not affect the response to sucrose.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2023)
Article
Substance Abuse
Julie A. Marusich, Jenny L. Wiley
Summary: This study examined the effect of different routes of administration on the potency and time course of THC's discriminative stimulus properties. The results showed that THC administered through various routes produced similar stimulus effects. These findings have implications for predicting THC's effects in humans.
DRUG AND ALCOHOL DEPENDENCE REPORTS
(2023)
