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Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases
Eur J Med Chem. 2024 Feb 3;268:116197. doi: 10.1016/j.ejmech.2024.116197. Online ahead of print.ABSTRACTDesloratadine, a second-generation histamine H1 receptor antagonist, has established itself as a first-line drug for the treatment of allergic diseases. Despite its effectiveness, desloratadine exhibits an antagonistic effect on muscarinic M3 receptor, which can cause side effects such as dry mouth and urinary retention, ultimately limiting its clinical application. Herein, we describe the discovery of compound Ⅲ-4, a novel H1 receptor antagonist with significant H1 receptor antagonistic activity (IC50 = 24.12 nM) and ...
Source: European Journal of Medicinal Chemistry - February 18, 2024 Category: Chemistry Authors: Zhaoxing Chu Lifang Cen Qinlong Xu Gaofeng Lin Jiajia Mo Li Shao Yan Zhao Jiaming Li Wenfeng Ye Tao Fang Weijie Ren Qihua Zhu Guangwei He Yungen Xu Source Type: research

Desloratadine alleviates ALS-like pathology in hSOD1 < sup > G93A < /sup > mice via targeting 5HTR < sub > 2A < /sub > on activated spinal astrocytes
In this study, we evaluated the therapeutic effects of desloratadine (DLT), a selective 5HTR2A antagonist, in human SOD1G93A (hSOD1G93A) ALS model mice, and elucidated the underlying mechanisms. HSOD1G93A mice were administered DLT (20 mg·kg-1·d-1, i.g.) from the age of 8 weeks for 10 weeks or until death. ALS onset time and lifespan were determined using rotarod and righting reflex tests, respectively. We found that astrocyte activation accompanying with serotonin receptor 2 A (5HTR2A) upregulation in the spinal cord was tightly associated with ALS-like pathology, which was effectively attenuated by DLT administration. ...
Source: Acta Pharmacologica Sinica - January 29, 2024 Category: Drugs & Pharmacology Authors: Jian Lu An-Xu He Zhuo-Ying Jin Meng Zhang Zhong-Xin Li Fan Zhou Lin Ma Hong-Ming Jin Jia-Ying Wang Xu Shen Source Type: research

Desloratadine alleviates ALS-like pathology in hSOD1G93A mice via targeting 5HTR2A on activated spinal astrocytes
Acta Pharmacologica Sinica, Published online: 29 January 2024; doi:10.1038/s41401-023-01223-2Desloratadine alleviates ALS-like pathology in hSOD1G93A mice via targeting 5HTR2A on activated spinal astrocytes (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 29, 2024 Category: Drugs & Pharmacology Authors: Jian Lu An-xu He Zhuo-ying Jin Meng Zhang Zhong-xin Li Fan Zhou Lin Ma Hong-ming Jin Jia-ying Wang Xu Shen Source Type: research

Hypersensitivity reaction to nedaplatin: A case report and literature review
Medicine (Baltimore). 2023 Dec 15;102(50):e36690. doi: 10.1097/MD.0000000000036690.ABSTRACTRATIONALE: Although rare, systemic hypersensitivity reactions to nedaplatin chemotherapy arise rapidly and can be life-threatening. The causes are unclear, and multiple potential mechanisms exist. Here, we report a case of systemic hypersensitivity reaction to nedaplatin and review the literature to establish a recommended protocol.PATIENT CONCERNS: A 62-year-old man was being treated for squamous lung cancer with multiple metastases. On the first day of chemotherapy, 5 minutes after nedaplatin infusion, he developed panic, shortness...
Source: Cancer Control - December 20, 2023 Category: Cancer & Oncology Authors: Kelun Gan Daiyuan Ma Source Type: research

Off-label Prescription in Paediatric Dermatology: A Retrospective Observational Study in a Tertiary Hospital
Acta Derm Venereol. 2023 Dec 11;103:adv11937. doi: 10.2340/actadv.v102.11937.ABSTRACTOff-label prescription in paediatric patients is common, where some studies indicate that dermatological conditions are more prone to off-label treatment. This is the first study to analyse the prevalence of off-label prescription in paediatric dermatology consultation. This retrospective observational study was performed using the medical records of paediatric patients who were evaluated in a paediatric dermatological consultation in Pontevedra University Hospital, Pontevedra, Spain. Of the 468 patients reviewed, 186 prescriptions were is...
Source: Acta Derm Venereol A... - December 11, 2023 Category: Dermatology Authors: Carmen Couselo-Rodr íguez Ana Batalla Sandra Mart ínez-Fernández Carmela D ávila-Pousa Diego Soto-Garc ía Luc ía Vilanova-Trillo Ángeles Flórez Source Type: research

Off-label Prescription in Paediatric Dermatology: A Retrospective Observational Study in a Tertiary Hospital
Acta Derm Venereol. 2023 Dec 11;103:adv11937. doi: 10.2340/actadv.v102.11937.ABSTRACTOff-label prescription in paediatric patients is common, where some studies indicate that dermatological conditions are more prone to off-label treatment. This is the first study to analyse the prevalence of off-label prescription in paediatric dermatology consultation. This retrospective observational study was performed using the medical records of paediatric patients who were evaluated in a paediatric dermatological consultation in Pontevedra University Hospital, Pontevedra, Spain. Of the 468 patients reviewed, 186 prescriptions were is...
Source: Acta Dermato-Venereologica - December 11, 2023 Category: Dermatology Authors: Carmen Couselo-Rodr íguez Ana Batalla Sandra Mart ínez-Fernández Carmela D ávila-Pousa Diego Soto-Garc ía Luc ía Vilanova-Trillo Ángeles Flórez Source Type: research

Hydroxypropyl Methylcellulose Orodispersible Film Containing Desloratadine for Geriatric Use: Formulation and Evaluation
(Source: Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry)
Source: Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry - December 6, 2023 Category: Allergy & Immunology Authors: Al-Oran, Aya Yahya F. Yenilmez, Evrim Tags: Research article Source Type: research