QPatch/Qube 384を用いた15報の論文が2021年第2四半期に発表されました。


15報のうち2報は、Sophionが心臓イオンチャネルの薬理学分野において執筆したものです。1報は東邦大学医学部薬理学教室との共同研究で、抗インフルエンザ薬として知られるオセルタミビルの抗心房細動作用を研究しました。もう1報は心臓安全性薬理分野のゴッドファーザーの一人であるBernard Fermini氏と弊社サイエンスディレクターであるDamian Bellが執筆した、安全性評価におけるAPCに関する幅広いレビューです。


In Jiang et al., Glenn King’s lab have published on a tarantula toxin that blocks Nav1.7 ion channels, showing its ability to reduce chronic visceral pain in irritable bowel syndrome (IBS).

Jensen et al., another paper involving the King lab in collaboration with Jennifer Deuis, Irina Vetter & Samuel Robinson’s labs, have done a deep dive into the venomous peptides of the velvet ant.

(研究機関一覧): YaleStanfordUniversity of UtahLundbeckGedeon RichterOrion PharmaBoehringer IngelheimPeking UniversityGuizhou UniversityESTEVEBarcelona Institute of Science & TechnologyAptuitTakedaNovartisLinköping UniversityUniversity of Chinese Academy of Sciences.

The velvet ant (Dasymutilla klugii) – from Jensen et al., U. Queensland



Kambayashi et al., 2021 Translational Studies on Anti-Atrial Fibrillatory Action of Oseltamivir by its in vivo and in vitro Electropharmacological Analyses

Jensen et al, 2021 Venom chemistry underlying the painful stings of velvet ants (Hymenoptera: Mutillidae)

Hopper et al., 2021 Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139

Bell, D.C. & Fermini, B., 2021 Use of automated patch clamp in cardiac safety assessment: past, present and future perspectives

Li et al., 2021 Identification of poly(ADP-ribose)polymerase 1 and 2 (PARP1/2) as targets of andrographolide using an integrated chemical biology approach

Schuelert et al., 2021 The Glycine Transport Inhibitor Bi 425809 Restores Translatable EEG Deficits in an Acute Mouse Model for Schizophrenia-Related Sensory Processing and Cortical Network Dysfunction

Paradkar et al., 2021 Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore

Ledneczki et al., 2021 HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor

Díaz et al., 2021 Tricyclic Triazoles as σ1Receptor Antagonists for Treating Pain

Barilli et al., 2021 From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents

Lapointe et al., 2021 Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.

Ottosson et al., 2021 Synthetic resin acid derivatives selectively open the hKV7.2/7.3 channel and prevent epileptic seizures.

Kong et al., 2021 Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens

Jiang et al., 2021 Pharmacological Inhibition of the Voltage-Gated Sodium Channel NaV1.7 Alleviates Chronic Visceral Pain in a Rodent Model of Irritable Bowel Syndrome

Zheng et al., 2021 Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain