Article
Neurosciences
Rawan S. Alnafisah, James Reigle, Mahmoud Ali Eladawi, Sinead M. O'Donovan, Adam J. Funk, Jaroslaw Meller, Robert E. Mccullumsmith, Rammohan Shukla
Summary: Antipsychotic drugs have a significant impact on postmortem studies of schizophrenia treatment. This study compares the effects of schizophrenia and antipsychotic drugs on the proteome to gain insight into the disease's pathophysiology. The findings reveal distinct changes in biological pathways, cell types, subcellular synaptic events, and drug targets between the two. The study identifies a hyperdopaminergic cortex and discusses the influence of drugs targeting cognitive symptoms on schizophrenia pathology.
NEUROPSYCHOPHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Jie Zhou, Cheng Peng, Qiuju Li, Xiaoyu Yan, Liang Yang, Mengting Li, Xiaoyu Cao, Xiaofang Xie, Dayi Chen, Chaolong Rao, Sizhou Huang, Fu Peng, Xiaoqi Pan
Summary: Aconitine exposure induces neurotoxicity and affects the dopaminergic system. Aconitine alters dopamine levels and activates the AC/cAMP/PKA pathway through dopamine receptors, disrupting intracellular calcium homeostasis and resulting in nerve cell damage.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Cell Biology
Kyoung Moo Choi, Andrew J. Haak, Ana M. Diaz Espinosa, Katherine A. Cummins, Patrick A. Link, Aja Aravamudhan, David K. Wood, Daniel J. Tschumperlin
Summary: The study identified critical downstream signaling elements linking GPCR agonism to YAP and TAZ inactivation in human lung fibroblasts. The signaling cascade involving EPAC1/2, RAP2c, and MAP4K7 is essential for the effects of dopamine D1 receptor agonism on fibroblast activities related to tissue repair and fibrosis. Targeted modulation of this cascade in fibroblasts may provide a useful strategy for regulating YAP and TAZ signaling.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Article
Biology
Natasha M. Puri, Giovanna R. Romano, Ting-Yu Lin, Quynh N. Mai, Roshanak Irannejad
Summary: This study demonstrates for the first time that dopamine D1 receptor (D1DR) can be activated at the Golgi apparatus in addition to its functions on the plasma membrane. The activation of Golgi-localized D1DR is dependent on organic cation transporter 2 (OCT2), providing an explanation for the access of membrane-impermeant dopamine to subcellular pools of D1DR. The study also reveals the role of Golgi-localized D1DR in regulating cAMP production and protein kinase A activation.
Article
Chemistry, Medicinal
Jun-Wei Xu, Yang-Li Qi, Jian-Wei Wu, Rui-Xiang Yuan, Xiao-Wen Chen, Jian-Qi Li
Summary: A series of potential antipsychotics were synthesized and evaluated, with compound 12a showing nanomolar affinity for specific receptors and demonstrating antipsychotic efficacy in an animal model. These compounds have potential as new antipsychotic drugs with good drug target selectivity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Medicine, Research & Experimental
Shannon E. Byrne, Nandini Vishwakarma, Srinivas Sriramula, Laxmansa C. Katwa
Summary: This article reviews the research on the role of dopamine receptors in cardiac tissue, with a particular focus on D3R. It summarizes the current state of knowledge and highlights areas of research that may be lacking. Additionally, it discusses the recent findings regarding the interaction between D3R and D1R.
Article
Biochemistry & Molecular Biology
Haolin Mo, Huixia Yu, Yang Li, Timothy P. C. Ezeorba, Zhihao Zhang, Mingxin Yao, Jiajia Yu, Dongmei Xiong, Haixia Liu, Lixin Wang
Summary: This study reports the molecular cloning, tissue distribution, and pharmacological characterization of the grass carp melanocortin-3-receptor (ciMC3R). The ciMC3R mRNA was found to be highly expressed in the brain of grass carp. Four agonists were shown to potentiate the activation of ciMC3R and further increase cAMP production and upregulate the MAPK/ERK signaling. This study provides basic data for exploring the physiological functions of grass carp MC3R, especially in energy homeostasis and food intake.
FISH PHYSIOLOGY AND BIOCHEMISTRY
(2023)
Review
Neurosciences
Nobuhisa Kanahara, Hiroshi Kimura, Yasunori Oda, Fumiaki Ito, Masaomi Iyo
Summary: Dopamine supersensitivity psychosis is a relatively rare clinical concept in schizophrenia patients, characterized by unstable mental state and tardive dyskinesia. It may lead patients to develop tolerance to antipsychotic medications and transition to treatment-resistant schizophrenia. Further research is needed to fully understand the implications of dopamine supersensitivity in schizophrenia treatment.
CURRENT NEUROPHARMACOLOGY
(2021)
Article
Neurosciences
Weiyuan Huang, Wanhong Zuo, Lixin Chen, Liwei Wang, George Tewfik, Rao Fu, Jiayi Zheng, Ding Li, Jiang-Hong Ye
Summary: Acetaldehyde exerts its aversive property by exciting LHb neurons via multiple cellular mechanisms and inducing conditioned place aversion. New treatments targeting LHb may be beneficial for alcoholism management.
JOURNAL OF NEUROSCIENCE
(2021)
Article
Cell Biology
Min-Che Tung, Yung-Wei Lin, Wei-Jiunn Lee, Yu-Ching Wen, Yu-Cheng Liu, Ji-Qing Chen, Michael Hsiao, Yi-Chieh Yang, Ming-Hsien Chien
Summary: Renal cell carcinoma (RCC) is a difficult-to-treat cancer, but recent research has found that penfluridol, a dopamine receptor D2 antagonist, can inhibit the growth of RCC cells and reduce their stemness through inducing autophagy-mediated apoptosis. This study suggests that penfluridol may be a potential therapeutic agent for treating RCC.
CELL DEATH & DISEASE
(2022)
Article
Neurosciences
Vindhya Nawaratne, Sean P. McLaughlin, Felix P. Mayer, Zayna Gichi, Alyssa Mastriano, Lucia Carvelli
Summary: The dopamine 2 receptors (D2R) play an important role in mediating the effects of amphetamine, which primarily rely on the ability of amphetamine to increase extracellular dopamine. This study found that prolonged exposure to amphetamine can decrease or increase endogenous hD2R at the cellular membrane in HEK293 cells. Moreover, the effects of amphetamine on D2R expression may occur independently of dopamine and DAT.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2021)
Article
Biochemistry & Molecular Biology
Dana R. Chambers, Agnieszka Sulima, Dan Luo, Thomas E. Prisinzano, Arthur E. Jacobson, Kenner C. Rice
Summary: The 5-(3-hydroxy)phenylmorphan structural class of compounds have an equatorially oriented aromatic ring and retain antinociceptive activity. The synthesized C9-alkyl diastereomers have been found to interact with opioid receptors and exhibit varying efficacy, including potent MOR agonists and a selective MOR antagonist that is more potent than naltrexone and antagonizes the EC90 of fentanyl to a greater extent.
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
Endocrinology & Metabolism
Federica Mangili, Donatella Treppiedi, Rosa Catalano, Giusy Marra, Genesio Di Muro, Anna Spada, Maura Arosio, Erika Peverelli, Giovanna Mantovani
Summary: FLNA is crucial for the expression and signaling of SSTR2 and DRD2 in GH- and PRL-secreting PitNETs. Its function is regulated by phosphorylation, with P-FLNA inhibiting SSTR2 antitumoral effects. Activation of cAMP pathway and DRD2 agonist can regulate FLNA activity by modulating its phosphorylation, affecting DRD2 signaling in tumoral pituitary cell lines.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Pharmacology & Pharmacy
Zhongtang Li, Fan Fang, Yiyan Li, Xuehui Lv, Ruqiu Zheng, Peili Jiao, Yuxi Wang, Guiwang Zhu, Zefang Jin, Xiangqing Xu, Yinli Qiu, Guisen Zhang, Zhongjun Li, Zhenming Liu, Liangren Zhang
Summary: This study reports a class of derivatives with dopamine D3 receptor selectivity as potential antipsychotic drugs. One compound, named 36b, exhibits multiple antipsychotic-like properties, including inhibiting excessive activity in mice, reducing climbing behavior, and demonstrating antidepressant-like activity, without adverse effects on mouse body weight and prolactin levels.
ACTA PHARMACEUTICA SINICA B
(2023)