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1.
J Cardiol Cases ; 27(2): 73-75, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36788956

RESUMO

Previous reports on cardiac intervention in cases with antithrombin deficiency are extremely limited. We report a case of acute coronary syndrome with antithrombin deficiency in a 62-year-old man with multiple histories of thrombosis. He had worsening chest pain, and laboratory data showed an elevated level of troponin T, suggesting acute myocardial infarction. Currently, there is no fixed anticoagulation strategy for coronary intervention in patients with antithrombin deficiency. In this case, we performed coronary intervention with heparin in addition to antithrombin concentrate. The intervention was successfully performed without thrombosis or bleeding complications. Learning objective: Antithrombin deficiency is a rare disorder and data about coronary intervention for cases with antithrombin deficiency are limited. We successfully performed intervention with our anticoagulant management and it would be beneficial for future reference.

2.
Bioorg Med Chem ; 26(15): 4410-4427, 2018 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-30031654

RESUMO

Since 6-prenylnaringenin (6-PNG) was recently identified as a novel T-type calcium channel blocker with the IC50 value around 1 µM, a series of flavanone derivatives were designed, synthesized and subsequently evaluated for T-channel-blocking activity in HEK293 cells transfected with Cav3.2 T-type channels using a patch-clamp technique. As a result, several new flavanones blocked Cav3.2-dependent T-currents more potently than 6-PNG. In the synthesized compounds, 6-(3-ethylpent-2-enyl)-5,7-dihydroxy-2-(2-hydroxyphenyl)chroman-4-one 8j, 6-(3-ethylpent-2-enyl)-5,7-dihydroxy-2-(4-hydroxyphenyl)chroman-4-one 11b, 6-(2-cyclopentylideneethyl)-5,7-dihydroxy-2-(4-hydroxyphenyl)chroman-4-one 11d, and 6-(2-Cyclopentylethyl)-5,7-dihydroxy-2-(4-hydroxyphenyl)chroman-4-one 12c were more potent blocker than 6-PNG with the IC50 value of 0.39, 0.26, 0.46, and 0.50 µM, respectively. Among the above four derivatives, the compound 8j provided the best result in the in vivo experiments; i.e. systemic administration of 8j at the minimum dose completely restored neuropathic pain induced by partial sciatic nerve ligation in mice.


Assuntos
Analgésicos/síntese química , Bloqueadores dos Canais de Cálcio/síntese química , Canais de Cálcio Tipo T/química , Desenho de Fármacos , Flavonoides/química , Potenciais de Ação/efeitos dos fármacos , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Bloqueadores dos Canais de Cálcio/farmacologia , Bloqueadores dos Canais de Cálcio/uso terapêutico , Canais de Cálcio Tipo T/metabolismo , Modelos Animais de Doenças , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Células HEK293 , Humanos , Concentração Inibidora 50 , Masculino , Camundongos , Neuralgia/tratamento farmacológico , Técnicas de Patch-Clamp , Relação Estrutura-Atividade
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