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26 results on '"Bian, Xiling"'

2. Pharmacological Activation of Neuronal Voltage-Gated Kv7/KCNQ/M-Channels for Potential Therapy of Epilepsy and Pain

Author

Liu, Yani, Bian, Xiling, Wang, KeWei, Barrett, James E., Editor-in-Chief, Flockerzi, Veit, Editorial Board Member, Frohman, Michael A., Editorial Board Member, Geppetti, Pierangelo, Editorial Board Member, Hofmann, Franz B., Editorial Board Member, Kuner, Rohini, Editorial Board Member, Michel, Martin C., Editorial Board Member, Page, Clive P., Editorial Board Member, Wang, KeWei, Editorial Board Member, Rosenthal, Walter, Editorial Board Member, and Gamper, Nikita, editor

Published
2021
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15. Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors

Author

Wang, Xintong, primary, Xiao, Haoran, additional, Wang, Jing, additional, Huang, Zongze, additional, Peng, Geng, additional, Xie, Wenjun, additional, Bian, Xiling, additional, Liu, Huijie, additional, Shi, Cheng, additional, Yang, Taoyi, additional, Li, Xin, additional, Gao, Jian, additional, Meng, Ying, additional, Jiang, Qianchen, additional, Chen, Wei, additional, Hu, Fang, additional, Wei, Ningning, additional, Wang, Xiaowei, additional, Zhang, Liangren, additional, Wang, KeWei, additional, and Sun, Qi, additional

Published
2021
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18. Visceral hyperalgesia induced by forebrain-specific suppression of native Kv7/KCNQ/M-current in mice

Author

Bian Xiling, Cao Xu, Su Jun, Chen Hui, Bi Yeping, and Wang KeWei

Subjects
forebrain, retigabine, XE-991, capsaicin, acetic acid, c-Fos, somatosensory cortex, Pathology, RB1-214
Abstract

Abstract Background Dysfunction of brain-gut interaction is thought to underlie visceral hypersensitivity which causes unexplained abdominal pain syndromes. However, the mechanism by which alteration of brain function in the brain-gut axis influences the perception of visceral pain remains largely elusive. In this study we investigated whether altered brain activity can generate visceral hyperalgesia. Results Using a forebrain specific αCaMKII promoter, we established a line of transgenic (Tg) mice expressing a dominant-negative pore mutant of the Kv7.2/KCNQ2 channel which suppresses native KCNQ/M-current and enhances forebrain neuronal excitability. Brain slice recording of hippocampal pyramidal neurons from these Tg mice confirmed the presence of hyperexcitable properties with increased firing. Behavioral evaluation of Tg mice exhibited increased sensitivity to visceral pain induced by intraperitoneal (i.p.) injection of either acetic acid or magnesium sulfate, and intracolon capsaicin stimulation, but not cutaneous sensation for thermal or inflammatory pain. Immunohistological staining showed increased c-Fos expression in the somatosensory SII cortex and insular cortex of Tg mice that were injected intraperitoneally with acetic acid. To mimic the effect of cortical hyperexcitability on visceral hyperalgesia, we injected KCNQ/M channel blocker XE991 into the lateral ventricle of wild type (WT) mice. Intracerebroventricular injection of XE991 resulted in increased writhes of WT mice induced by acetic acid, and this effect was reversed by co-injection of the channel opener retigabine. Conclusions Our findings provide evidence that forebrain hyperexcitability confers visceral hyperalgesia, and suppression of central hyperexcitability by activation of KCNQ/M-channel function may provide a therapeutic potential for treatment of abdominal pain syndromes.

Published
2011
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19. Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice

Author

Li, Yuanheng, primary, Sun, Lilan, additional, Yang, Taoyi, additional, Jiao, Wenxuan, additional, Tang, Jingshu, additional, Huang, Xiaomin, additional, Huang, Zongze, additional, Meng, Ying, additional, Luo, Laichun, additional, Wang, Xintong, additional, Bian, Xiling, additional, Zhang, Fang, additional, Wang, KeWei, additional, and Sun, Qi, additional

Published
2018
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20. Allosteric Activation of α7 Nicotinic Acetylcholine Receptors by Novel 2-Arylamino-thiazole-5-carboxylic Acid Amide Derivatives for the Improvement of Cognitive Deficits in Mice

Author

Yang, Chenxia, Meng, Ying, Wang, Xintong, Li, Xin, Yu, Tong, Liao, Weiming, Xie, Wenjun, Jiang, Qianchen, Wang, Han, Shi, Cheng, Jiao, Wenxuan, Bian, Xiling, Hu, Fang, Wang, Xiaowei, Liu, Yani, Zhang, Liangren, Wang, KeWei, and Sun, Qi

Abstract

Enhancing α7 nAChR function serves as a therapeutic strategy for cognitive disorders. Here, we report the synthesis and evaluation of 2-arylamino-thiazole-5-carboxylic acid amide derivatives 6–9that as positive allosteric modulators (PAMs) activate human α7 nAChR current expressed in Xenopusooctyes. Among the 4-amino derivatives, a representative atypical type I PAM 6pexhibits potent activation of α7 current with an EC50of 1.3 μM and the maximum activation effect on the current over 48-fold in the presence of acetylcholine (100 μM). The structure–activity relationship (SAR) analysis reveals that the 4-amino group is crucial for the allosteric activation of α7 currents by compound 6pas the substitution of 4-methyl group results in its conversion to compound 7b(EC50= 2.1 μM; max effect: 58-fold) characterized as a typical type I PAM. Furthermore, both 6pand 7bare able to rescue auditory gating deficits in mouse schizophrenia-like model of acoustic startle prepulse inhibition.

Published
2024
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22. Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice

Author

Li, Yuanheng, Sun, Lilan, Yang, Taoyi, Jiao, Wenxuan, Tang, Jingshu, Huang, Xiaomin, Huang, Zongze, Meng, Ying, Luo, Laichun, Wang, Xintong, Bian, Xiling, Zhang, Fang, Wang, KeWei, and Sun, Qi

Abstract

A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones (3aa–3eq) were designed, synthesized, and evaluated as the type I positive allosteric modulators of human α7 nAChR expressed in Xenopusooctyes by a two-electrode voltage clamp. The structure–activity relationship analysis identified the compound 3eaas a potent and efficacious PAM with the maximum activation effect of the α7 current of over 1633% in the presence of acetylcholine (100 μM) and an EC50= 1.26 μM. It is highly specific to α7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABAAreceptors. Compound 3eashowed an elimination half-life of 10.8 ± 1.5 h for 3 mg/kg, i.v., and 7.4 ± 1.1 h for 60 mg/kg, i.g. in rat. It also exhibited sufficient blood–brain barrier penetration with no significant effect on hERG channel. Most importantly, compound 3eadose-dependently (0.1–1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model.

Published
2019
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