Review
Biochemistry & Molecular Biology
Kavya Prasad, Erik F. J. de Vries, Philip H. Elsinga, Rudi A. J. O. Dierckx, Aren van Waarde
Summary: Adenosine and dopamine interact antagonistically in living mammals via adenosine A(2A) and dopamine D-2 receptors. These interactions mainly occur in striatal neurons and astrocytes, and may have therapeutic potential for Parkinson's disease, schizophrenia, substance abuse, and attention deficit-hyperactivity disorder.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Sabrina Biselli, Merlin Bresinsky, Katharina Tropmann, Lisa Forster, Claudia Honisch, Armin Buschauer, Gunther Bernhardt, Steffen Pockes
Summary: A series of novel H2R and D3R agonists with high affinities and selectivity have been synthesized in this study, showing promising application prospects in in vitro experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Wen-Ling Dai, Yi-Ni Bao, Ji-Fa Fan, Bin Ma, Shan-Shan Li, Wan-Li Zhao, Bo-Yang Yu, Ji-Hua Liu
Summary: The study demonstrates that D1DR and D2DR antagonists reduce NMDAR-mediated spinal neuron activation, alleviate bone cancer pain, and act through the Gq protein and Src pathways.
JOURNAL OF ADVANCED RESEARCH
(2021)
Article
Neurosciences
Yasuharu Yamamoto, Keisuke Takahata, Manabu Kubota, Harumasa Takano, Hiroyoshi Takeuchi, Yasuyuki Kimura, Yasunori Sano, Shin Kurose, Hiroshi Ito, Masaru Mimura, Makoto Higuchi
Summary: The study revealed a significant positive correlation between DA synthesis capacity and DA transporter availability in the putamen, but no significant correlation between DA synthesis capacity and D2 receptor availability in the striatum, indicating a relationship between DA synthesis capacity and reuptake, while the total abundance of D2 receptors may not directly participate in the regulatory mechanism.
Article
Chemistry, Medicinal
Gui-Long Tian, Chia-Ju Hsieh, Michelle Taylor, Aladdin A. Riad, Robert R. Luedtke, Robert H. Mach
Summary: The difference in the secondary binding site between D2R and D3R has been utilized to design compounds with selectivity for D3R. This study prepared a series of bitopic ligands based on Fallypride to improve the selectivity for D3R using various secondary binding fragments. The results showed that compounds with a small alkyl group containing a heteroatom exhibited improved D3R selectivity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Ophthalmology
Furong Huang, Ziheng Shu, Qin Huang, Kaijie Chen, Wenjun Yan, Wenjing Wu, Jinglei Yang, Qiongsi Wang, Fengjiao Wang, Chunlan Zhang, Jia Qu, Xiangtian Zhou
Summary: This study investigates the locations of dopamine D2 receptors (D2Rs) that regulate form-deprivation myopia (FDM) using different transgenic mouse models. The findings suggest that D2Rs located in the retina play a role in the dopaminergic regulation of FDM in mice.
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
(2022)
Review
Pharmacology & Pharmacy
Mattia Ferraiolo, Emmanuel Hermans
Summary: L-DOPA and dopamine agonists are key therapeutic options for managing the motor symptoms of Parkinson's disease. Despite similarities in their mechanism of action, pramipexole, ropinirole, and rotigotine have distinct clinical profiles possibly due to differences in their pharmacological properties. This review aims to explore the properties of these dopamine agonists from both clinical and molecular perspectives, providing a unified framework for interpretation.
PHARMACOLOGY & THERAPEUTICS
(2023)
Article
Oncology
Arely Rosas-Cruz, Nohemi Salinas-Jazmin, Anahi Valdes-Rives, Marco A. Velasco-Velazquez
Summary: This study analyzed the expression of dopamine receptors (DRs) in breast cancer and their functional role in cancer stem cells (CSCs). The results showed that DRD4 was overexpressed and had prognostic value in breast tumors. DRD1 and DRD4 were found to be relevant in stemness control of CSCs. Additionally, DRD4 inhibition increased CSCs content and reduced cell migration.
TRANSLATIONAL CANCER RESEARCH
(2022)
Review
Peripheral Vascular Disease
Masaki Mogi
Summary: Aldosterone breakthrough is a phenomenon that occurs in hypertensive patients who have been on long-term RAAS blockade, where blood pressure remains uncontrolled despite the use of antihypertensive drugs. This puts patients at higher risk of cardiovascular disease and worsens prognosis.
HYPERTENSION RESEARCH
(2022)
Article
Plant Sciences
Han Zhou, Tao Hou, Zhenhua Gao, Xiujie Guo, Chaoran Wang, Jixia Wang, Yanfang Liu, Xinmiao Liang
Summary: This study isolated eight alkaloids from lotus leaves and evaluated them on dopamine receptors. These alkaloids acted as antagonists for D1 and D2 receptors, with O-nornuciferine being the most potent among the eight on both receptors.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Daiki Masukawa, Satoshi Kitamura, Rei Tajika, Hiraku Uchimura, Masami Arai, Yuuki Takada, Tetsu Arisawa, Momoyo Otaki, Kaori Kanai, Kenta Kobayashi, Tomoyuki Miyazaki, Yoshio Goshima
Summary: Dopamine (DA) is involved in neurological and physiological functions such as motor control. L-3,4-dihydroxyphenylalanine (L-DOPA), traditionally seen as an inert precursor of DA, is now shown to be a neurotransmitter itself.
JOURNAL OF NEUROCHEMISTRY
(2023)
Article
Neurosciences
Perla Ugalde-Muniz, Maria Guadalupe Hernandez-Luna, Stephany Garcia-Velasco, Rafael Lugo-Huitron, Jimena Murcia-Ramirez, Ricardo Jesus Martinez-Tapia, Roxana Noriega-Navarro, Luz Navarro
Summary: The proinflammatory state induced by sleep deprivation plays a crucial role in the development of neurodegenerative processes. This study reveals that activation of dopamine D2 receptors can attenuate the proinflammatory response and memory impairment caused by REM sleep deprivation.
FRONTIERS IN NEUROSCIENCE
(2022)
Review
Chemistry, Medicinal
Radomir Juza, Kamil Musilek, Eva Mezeiova, Ondrej Soukup, Jan Korabecny
Summary: Dopamine, a biologically active amine, acts by activating dopamine receptors in the nervous system. This review discusses the pharmacophore and critical moieties for high D2R affinity and summarizes the therapeutic potential of D2R modulators in schizophrenia, Parkinson's disease, depression, and anxiety. It also provides an overview of the dopaminergic pathway underlying these disorders.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Anatomy & Morphology
Joseph J. Lebowitz, Mason Trinkle, James R. Bunzow, Judith Joyce Balcita-Pedicino, Savas Hetelekides, Brooks Robinson, Santiago De la Torre, Sue A. Aicher, Susan R. Sesack, John T. Williams
Summary: This study utilized advanced microscopy techniques to observe the distribution of D2 receptors in dopamine neurons and found that membrane-bound D2 receptors are densely distributed in specific areas, providing a quantitative estimate of spatial frequency for the first time.
BRAIN STRUCTURE & FUNCTION
(2022)
Review
Medicine, General & Internal
Nasimudeen R. Jabir, Chelapram K. Firoz, Torki A. Zughaibi, Mohammed Abdullah Alsaadi, Adel M. Abuzenadah, Ahmed Ibrahim Al-Asmari, Ahdab Alsaieedi, Bakrudeen Ali Ahmed, Arun Kumar Ramu, Shams Tabrez
Summary: Yohimbine is a phytochemical that has significant pharmacological potential and is being extensively researched. It acts on both the central and peripheral nervous systems, selectively blocking α2-adrenergic receptors. Yohimbine also shows therapeutic potential against human diseases, but further research is needed.
ANNALS OF MEDICINE
(2022)
Article
Oncology
Jacqueline E. Reilly, Jeffrey D. Neighbors, Raymond J. Hohl
CANCER BIOLOGY & THERAPY
(2017)
Article
Orthopedics
Jeff W. Stevens, David K. Meyerholz, Jeffery D. Neighbors, Jose A. Morcuende
JOURNAL OF ORTHOPAEDIC RESEARCH
(2018)
Article
Endocrinology & Metabolism
Jillian S. Weissenrieder, Jacqueline E. Reilly, Jeffrey D. Neighbors, Raymond J. Hohl
Article
Oncology
Kathleen M. Kokolus, Jeremy S. Haley, Emily J. Koubek, Raghavendra Gowda, Saketh S. Dinavahi, Arati Sharma, David F. Claxton, Klaus F. Helm, Joseph J. Drabick, Gavin P. Robertson, Jeffrey D. Neighbors, Raymond J. Hohl, Todd D. Schell
Article
Clinical Neurology
Xuemei Huang, Nicholas W. Sterling, Guangwei Du, Dongxiao Sun, Christina Stetter, Lan Kong, Yusheng Zhu, Jeffery Neighbors, Mechelle M. Lewis, Honglei Chen, Raymond J. Hohl, Richard B. Mailman
MOVEMENT DISORDERS
(2019)
Article
Pharmacology & Pharmacy
Jillian S. Weissenrieder, Jessie L. Reed, Michelle Green, George-Lucian Moldovan, Emily J. Koubek, Jeffrey D. Neighbors, Raymond J. Hohl
Article
Pharmacology & Pharmacy
Jillian S. Weissenrieder, Jessie L. Reed, George-Lucian Moldovan, Martin T. Johnson, Mohamed Trebak, Jeffrey D. Neighbors, Richard B. Mailman, Raymond J. Hohl
Summary: D-2 receptor antagonists are potential anticancer therapeutics with specific utility for CNS cancers, but the cytotoxicity they induce in GBM cell lines is associated with calcium signaling mechanisms, not D2R antagonism. Repurposing of existing drugs should focus on targeting calcium flux rather than D2R antagonism.
PHARMACOLOGY RESEARCH & PERSPECTIVES
(2021)
Article
Multidisciplinary Sciences
J. S. Weissenrieder, J. D. Weissenkampen, J. L. Reed, M. V. Green, C. Zheng, J. D. Neighbors, D. J. Liu, Raymond J. Hohl
Summary: The natural compounds of the schweinfurthin family have potent cytotoxicity against various cancer cell lines, but the precise mechanism of action remains unknown. This study used RNA sequencing to analyze the gene expression patterns in cells treated with a schweinfurthin analog, revealing differential regulation of metabolic and stress-response pathways between sensitive and resistant cell lines. The Hedgehog pathway was found to be differentially regulated in the resistant cell line, suggesting its involvement in resistance to schweinfurthin treatment. This study identifies a key interaction between the Hedgehog pathway and the sensitivity to schweinfurthin compounds.
SCIENTIFIC REPORTS
(2022)
Article
Virology
Emily J. Koubek, Jillian S. Weissenrieder, Luz E. Ortiz, Nnenna Nwogu, Alexander M. Pham, J. Dylan Weissenkampen, Jessie L. Reed, Jeffrey D. Neighbors, Raymond J. Hohl, Hyun Jin Kwun
Summary: Merkel cell carcinoma (MCC) is an aggressive form of skin cancer caused by the Merkel cell polyomavirus (MCPyV). A recent study found that schweinfurthin compounds can selectively inhibit MCPyV-infected cancer cell lines and induce apoptosis. This discovery suggests a promising new therapeutic option for virus-induced MCC.
Article
Biochemistry & Molecular Biology
Sara Danielli, Zhongming Ma, Eirini Pantazi, Amrendra Kumar, Benjamin Demarco, Fabian A. Fischer, Usha Paudel, Jillian Weissenrieder, Robert J. Lee, Sebastian Joyce, J. Kevin Foskett, Jelena S. Bezbradica
Summary: CALHM6, a membrane ion channel, promotes cell-cell crosstalk at neuronal synapses via ATP release and is highly expressed in immune cells. It has been linked to NK cell anti-tumor activity, but its mechanism of action and broader functions in the immune system remain unclear.
Review
Biochemistry & Molecular Biology
Emily J. Koubek, Jillian S. Weissenrieder, Jeffrey D. Neighbors, Raymond J. Hohl