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Discovery of Trace Amine Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4H-1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders
Biomolecules. 2022. Vol. 12. No. 11. Article 1650.
Krasavin M., Lukin A., Sukhanov I., Gerasimov A., Kuvarzin S., Efimova E., Dorofeikova M., Maxim Gureev
A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenethylamine (PEA) or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely related hits displaying EC50 values in the upper submicromolar range. Extensive analog synthesis and testing for TAAR1 agonism in a BRET-based cellular assay identified compound 62 (LK00764) with EC50 = 4.0 nM. The compound demonstrated notable efficacy in such schizophrenia-related in vivo tests as MK-801-induced hyperactivity and spontaneous activity in rats, locomotor hyperactivity of dopamine transporter knockout (DAT-KO) rats, and stress-induced hyperthermia (i.p. administration). Further preclinical studies are necessary to evaluate efficacy, safety and tolerability of this potent TAAR1 agonist for the potential development of this compound as a new pharmacotherapy option for schizophrenia and other psychiatric disorders.
Springer, 2026.
This book highlights cutting-edge research in the field of network science, offering scientists, researchers, students and practitioners a unique update on the latest advances in theory and a multitude of applications. It presents the peer-reviewed proceedings of the XIV International Conference on Complex Networks and their Applications (COMPLEX NETWORKS 2025). The carefully selected papers cover ...
Added: October 13, 2026
Springer, 2026.
This book offers a comprehensive overview of the latest research, innovations, and practical applications in the field of sustainability, with a focus on construction materials and their use in building and civil engineering structures. As an outcome of the 3rd International Conference on Sustainability: Developments and Innovations (ICSDI 2026), this book presents a selection of ...
Added: October 13, 2026
Dmitriev A., Kornilov V., Batienkov R., Lecture Notes in Civil Engineering 2026 Vol. 886 P. 249–255
Numerous studies have provided compelling evidence that the probability distribution of avalanche sizes follows a power law, and that 1/f noise is present in the stochastic dynamics of landslides. We present a theoretical explanation of these phenomena within the framework of self-organized criticality theory, proposing a discrete-time model in the form of a sandpile cellular ...
Added: October 13, 2026
Dmitriev A., Shulman I., Lebedev A., Studies in Computational Intelligence 2026 Vol. 1265 P. 266–273
A discrete-time model is presented for the self-organization of the X/Twitter social network to the edge of a phase transition, characterized by avalanche-like propagation of information in the network. The model is based on the analogy between the critical dynamics of the X social network and sandpile cellular automata with Manna rule on the Chung-Lu ...
Added: October 13, 2026
Makarov D. M., Kalikin N., Fashchevsky K. A. et al., Electrochimica Acta 2026 Vol. 579 Article 150159
Machine learning (ML) has become a powerful tool for accelerating the development of carbon-based supercapacitors;
however, most published models assume that a single predictive framework can describe both conventional
porous carbons and hybrid carbon electrodes. Here, we test this assumption using a comprehensive
benchmark dataset and an extended literature-curated dataset enriched with synthesis- and electrolyte-related
descriptors. Three ML algorithms ...
Added: October 13, 2026
Zhang Z., Ilvovsky D., Information Processing and Management 2026 Vol. 63 No. 7
Transformer-based Large Language Models (LLMs) rely on Key-Value (KV) cache to accelerate autoregressive decoding, but memory and compute requirements still grow with context length, limiting deployment on resource-constrained devices. Existing training-free KV cache compression methods mainly rely on attention-driven retention heuristics, which may under preserve structurally informative tokens under tight cache budgets, especially when such ...
Added: October 13, 2026
Батова О. Н., Савинецкая Л. Е., Проявка С. В. et al., Nature Conservation Research. Заповедная наука 2026 Т. 11 № 4 С. 25–39
Spermophilus suslicus is a threatened species listed in Red Data Books at all levels (from regional Red Data
Books to the IUCN Red List of Threatened Species), and it currently requires special conservation activity.
Over the past 30–50 years, its range has changed from continuous to mosaic, and its population has declined
everywhere. In 2015, in Russia experimental ...
Added: October 13, 2026
No Species Is an Island, Entire of Itself: Genetic Speciation Algorithm with Interplay among Species
International Journal of Engineering, Transactions B: Applications 2027 Vol. 40 No. 5 P. 1437–1460
This paper, with a particular emphasis on Genetic Algorithm (GA), proposes a novel approach that integrates clustering mechanisms, predator-prey dynamics, and a distinctive selection strategy for generating subsequent populations. The proposed evolutionary algorithm, referred to as Genetic Speciation Algorithm with Interplay Among Species (GSAIS), is comprehensively evaluated against several variants of GAs as well as ...
Added: October 12, 2026
Alexandrov D., Vasilevsky V., Rezunik L. et al., Труды Института системного программирования РАН 2026 Т. 38 № 5 С. 73–90
Large language models demonstrate limitations in tasks that require precise information retrieval from very long input sequences. This limitation affects code generation in large object-oriented systems, where correctness depends on complex inter-class dependencies and the analysis of long execution traces that exceed standard context window sizes. This paper presents JavaCapsule, a technology for automated generation ...
Added: October 12, 2026
Singapore: Springer, 2026.
This volume presents the Proceedings of the 34th IUPAP Conference on Computational Physics (CCP2023), held in Kobe, Japan on August 4–8, 2023. It offers a collection of peer-reviewed articles that highlight recent developments in computational and simulation research across various areas of physics. Key topics include the use of data science, quantum computing, and machine ...
Added: October 12, 2026
Zykov S. V., Ермаков С. Р., Современные наукоемкие технологии 2026 № 9 С. 43–53
При федеративном обучении с неоднородными клиентскими данными и переменными задержками запоздавшие обновления могут ухудшать качество модели, а обмен параметрами с глобальным сервером увеличивает сетевую нагрузку. Целью исследования является разработка и теоретико-экспериментальное обоснование метода и алгоритмов адаптивного федеративного обучения с учетом распределенного запаздывания клиентских обновлений. Для обоснования разрабатываемых решений использованы событийная и непрерывная модели градиентных обновлений, ...
Added: October 11, 2026
Temereva E., Zoologischer Anzeiger 2026 Vol. 325 P. 182–195
Brachiopoda is a group of animals, that is still insufficiently studied at the ultrastructural level, despite the significance of ultrastructure of tissues and organs for analysing the functional morphology, reconstructing the organisation and biology of numerous extinct brachiopods, and establishing relationships among major taxa. In the present study, we provide a revised reconstruction of the ...
Added: October 11, 2026
Shi R., Yu Y., Chibisov A., International Journal of Hydrogen Energy 2025 Vol. 107 P. 52–62
Cyanide containing wastewater can cause livestock death and reduce agricultural production and electrochemical reduction of cyanide (CNRR) is a promising way to eliminate its harm and turn waste into valuable products. However, the reaction mechanism and function of electrocatalysts for CNRR have not been fully understood yet. Herein we identify a two-dimensional (2D) conductive copper-organic ...
Added: October 11, 2026
Брычков М. Е., Незнанов А.А., Программирование 2026 № 4 С. 50–66
The matrix profile (MP) quickly became one of the most important time series preprocessing methods when it was introduced in 2016, facilitating the solution of a wide range of time series analysis problems, in particular anomaly and pattern detection problems. The high significance has led to the emergence of various tools for MP calculating, but ...
Added: October 9, 2026
Aleskerov F. T., Вайншток А. П., Делахова А. М. et al., Информационные процессы 2026 Т. 26 № 3 С. 895–913
The development and effective management of territorial entities are priority issues for all states, particularly in the context of the digital transformation of public administration. Over the past decade, the integration of information technologies into municipal and regional planning has significantly altered approaches to strategic development, service delivery, and public engagement. This paper describes the ...
Added: October 9, 2026
Stepanyants V., Andrey V. Fizulin, Chibirov A. et al., FUTURE TRANSPORTATION 2026 Vol. 6 No. 5 Article 225
Reliable Vehicle-to-Everything (V2X) evaluation requires propagation models that represent terrain and multilevel infrastructure. Most integrated vehicular simulators still rely on planar models, but the magnitude of the resulting bias is unclear. This study quantitatively compares flattened two-dimensional (2D) and terrain-aware three-dimensional (3D) variants of three scenarios using identical Sionna RT settings. The pipeline combines OpenStreetMap ...
Added: October 8, 2026
Люксембург А. А., УРСС, 2005.
Изучается возможность автоматизированного построения математических теорий. Рассматривается дедуктивная система, основанная на языке логики предикатов первого порядка, объектами системы являются математические выражения или формулы, которые описывают математические объекты или их свойства. В дедуктивной системе выводятся математические определения и теоремы. Для доказательства теорем используются методы автоматического доказательства. Разработан алгоритм, выводящий часть формул системы. Для решения задачи используется аппарат математической ...
Added: October 7, 2026
Groshev Maksim, Rybakov Petr, Teterin N. et al., Sensors 2026 Article 6171
Manual assessment of soybean yield components, such as pod number, is laborious, time-consuming, and subjective. Existing computer-vision approaches based on object detection or instance segmentation perform poorly on close-range RGB imagery of soybean canopies due to severe occlusions, ambiguous plant boundaries, and the high cost of bounding-box annotation. To address these challenges, we propose a ...
Added: October 7, 2026
Кияненко И. К., Клиническая и специальная психология 2026 Т. 15 № 1 С. 7–19
Context and relevance. The problem of the impact of urban stress factors on mental health is becoming increasingly relevant in the context of urbanization. Living in cities is accompanied by increased psychophysiological stress, which leads to an increase in the prevalence of mental disorders among urban residents. Objective. The purpose of the article is to ...
Added: May 19, 2026
Petrova D., Biomolecules 2025
Added: January 18, 2026
Alexey M. Dvoinin, Kopeyko G., Borisova O. et al., Frontiers in Psychiatry 2025 No. 16 Article 1553990
Introduction: As demonstrated in previous research and clinical observations, the personal value system is subject to disintegration as a consequence of schizophrenia. Patients with schizophrenia are sometimes religious and use religious coping mechanisms. A number of studies emphasize the benefits of positive religious coping as a part of clinical treatment for patients with schizophrenia and ...
Added: April 7, 2025
Белоусова А. Ю., Зотова Н. Е., Korotkova I., Вестник психотерапии 2025 № 93 С. 100–112
Relevance. Social cognition impairments in patients with schizophrenia complicate their interactions with others, adversely impacting daily functioning and the progression of the disease. Investigating these impairments is crucial for developing effective strategies for diagnosis, rehabilitation, and psychological intervention to improve patients’ quality of life.
Intention. To investigate the impairments in cognitive information processing in patients with ...
Added: April 7, 2025
Касьянов Е., Пинахина Д., Rakitko A. et al., Consortium Psychiatricum 2024 Vol. 5 No. 2 P. 5–15
Added: November 10, 2024
Олейчик И. В., Баранов П. А., Shishkovskaya T. et al., Современная терапия психических расстройств 2021 № 2 С. 28–35
Актуальность. По данным целого ряда исследований, депрессии при шизофрении регистрируются в среднем у 25 % больных и по показате5 лям распространенности в структуре данного заболевания уступают лишь галлюцинаторно5параноидной и негативной симптоматике. При этом данные состояния вообще не указываются в качестве отдельного показания к назначению психофармакологических средств, хотя в условиях реальной клинической практики они, несомненно, требуют ...
Added: March 12, 2024