腺苷 A3 受体激活药物对癫痫组织的选择性调节

IF 6.8 2区医学 Q1 PHARMACOLOGY & PHARMACY British Journal of Pharmacology Pub Date : 2024-09-19 DOI:10.1111/bph.17319

Anwesha Ghosh, Leonor Ribeiro-Rodrigues, Gabriele Ruffolo, Veronica Alfano, Cátia Domingos, Nádia Rei, Dilip K. Tosh, Diogo M. Rombo, Tatiana P. Morais, Cláudia A. Valente, Sara Xapelli, Beatriz Bordadágua, Alexandre Rainha-Campos, Carla Bentes, Eleonora Aronica, Maria José Diógenes, Sandra H. Vaz, Joaquim A. Ribeiro, Eleonora Palma, Kenneth A. Jacobson, Ana M. Sebastião

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引用次数: 0

摘要

腺苷通过 A1 受体（A1R）是一种内源性抗惊厥药。腺苷受体激动剂作为抗癫痫药物的开发一直受到其心脏副作用的阻碍。据报道，一种中度 A1R 选择性激动剂 MRS5474 可抑制癫痫发作，但不会对心脏产生很大影响。我们推测这种药物可能通过 A1R 以外的途径和/或特定疾病机制发挥作用，因此我们评估了 MRS5474 对海马的影响。

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Selective modulation of epileptic tissue by an adenosine A3 receptor-activating drug

Adenosine, through the A₁ receptor (A₁R), is an endogenous anticonvulsant. The development of adenosine receptor agonists as antiseizure medications has been hampered by their cardiac side effects. A moderately A₁R-selective agonist, MRS5474, has been reported to suppress seizures without considerable cardiac action. Hypothesizing that this drug could act through other than A₁R and/or through a disease-specific mechanism, we assessed the effect of MRS5474 on the hippocampus.

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来源期刊

British Journal of Pharmacology 医学-药学

CiteScore

15.40

自引率

12.30%

发文量

270

审稿时长

2.0 months

期刊介绍： The British Journal of Pharmacology (BJP) is a biomedical science journal offering comprehensive international coverage of experimental and translational pharmacology. It publishes original research, authoritative reviews, mini reviews, systematic reviews, meta-analyses, databases, letters to the Editor, and commentaries. Review articles, databases, systematic reviews, and meta-analyses are typically commissioned, but unsolicited contributions are also considered, either as standalone papers or part of themed issues. In addition to basic science research, BJP features translational pharmacology research, including proof-of-concept and early mechanistic studies in humans. While it generally does not publish first-in-man phase I studies or phase IIb, III, or IV studies, exceptions may be made under certain circumstances, particularly if results are combined with preclinical studies.