布拉地新钠(Bucladesine Sodium) - 药物靶点：cGMP-PDE_在研适应症：褥疮，皮肤溃疡，心室功能不全_专利_临床

概要

基本信息

药物类型

小分子化药

别名

3',5'-cyclic AMP dibutyrate、Bucladesine、Bucladesine sodium (JAN)

+ [17]

靶点

cGMP-PDE

作用方式

抑制剂

作用机制

cGMP-PDE抑制剂(cGMP-磷酸二酯酶抑制剂)

治疗领域

心血管疾病皮肤和肌肉骨骼疾病

在研适应症

褥疮皮肤溃疡心室功能不全

非在研适应症-

原研机构

Alfresa Pharma Corp.

在研机构

Alfresa Pharma Corp.Nipro Pharma Corp.

非在研机构-

权益机构

Daiichi Sankyo Co., Ltd.

Alfresa Pharma Corp.

最高研发阶段批准上市

首次获批日期

日本 (1984-07-24),

心室功能不全

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C18H24N5NaO8P

InChIKeyWAOODRHZYQRSDS-JBVYASIDSA-N

CAS号16980-89-5

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关联

2

项与布拉地新钠相关的临床试验

CTR20233188

/ Not yet recruitingN/A

评价注射用二丁酰环磷腺苷钠在中国成年健康受试者中的一项单中心、随机、开放条件下单次给药、两制剂、两周期交叉的生物等效性研究

主要研究目的：考察单次静脉泵入300mg受试制剂注射用二丁酰环磷腺苷钠和参比制剂注射用二丁酰环磷腺苷钠在中国成年健康受试者体内的药代动力学特征，初步评估两种制剂的生物等效性。次要研究目的：评价单次静脉泵入300mg受试制剂和参比制剂在中国成年健康受试者中的安全性。

开始日期-

申办/合作机构

湖南尔康制药股份有限公司

JPRN-jRCT2041210065

/ Recruiting临床1/2期IIT

A Phase I/II Multi-Institutional Study of Bucladesine in Patients with Severe Methylmalonic Acidemia - McAMP

开始日期2022-03-10

申办/合作机构-

100 项与布拉地新钠相关的临床结果

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100 项与布拉地新钠相关的转化医学

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100 项与布拉地新钠相关的专利（医药）

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10,293

项与布拉地新钠相关的文献（医药）

2025-04-01·Theriogenology

Melatonin and cyclic adenosine monophosphate enhance the meiotic and developmental competence of porcine oocytes from early antral follicles during in vitro growth and pre-maturation culture

Article

作者: Bui, Hong-Thuy ; Huyen, Truong Thi Ngoc ; Thien, Lam Chi ; Minh, Do Tu ; Minh, Nguyen Uyen ; Phuong, Lam Do Truc ; Thien Truc, Le Nguyen ; Su Pham, Cao Dang ; Huy Bao, Nguyen Thai ; Van Thuan, Nguyen ; Nguyen, Nhat-Thinh

Melatonin has been studied for its ability to improve oocyte quality and modulate cyclic adenosine monophosphate (cAMP) production. However, the effects of melatonin on the in vitro growth (IVG) of oocyte-cumulus-granulosa complexes (OCGCs) derived from early antral follicles (EAFs) have not been fully investigated. This study aimed to examine the effects of melatonin during IVG on the developmental competence and blastocyst quality of porcine oocytes isolated from EAFs. In addition, the combination of melatonin with dibutyl cAMP (Mela + dbcAMP) or hypoxanthine (Mela + HX) during IVG and pre-in vitro maturation (pre-IVM) was also investigated. The result showed that the modified medium supplemented with 10 μM melatonin after 4-day IVG enhanced antrum formation, survival rate, and oocyte diameter, especially, the melatonin-treated group enhanced expression of histone acetylation (Ac-H3-K9) higher than the untreated group. In addition, the combination of 10 μM melatonin with dbcAMP during IVG and during 7h of pre-IVM had significantly improved meiotic competence and cumulus expansion after IVM compared to Mela + HX groups. Finally, the combination of Mela + dbcAMP improved parthenogenetic blastocyst formation rather than the untreated group, and expression of histone methylation (Me-H3-K4) and Ac-H3-K9 in blastocyst comparable group derived from oocytes of large antral follicles (LAFs). Furthermore, melatonin with concentrations of 10 μM and 100 μM during IVG enhanced expression of pluripotency gene-related (OCT4, NANOG, SOX2) and balance cell viability via apoptosis-related gene (BCL2/BAX). In conclusion, melatonin combined with dbcAMP during IVG and pre-IVM of oocytes derived from EAFs demonstrated superior efficacy in enhancing oocyte growth, maturation, and development of porcine pre-implantation embryos.

2025-03-01·Food Chemistry

Analysis of changes in flavor characteristics of congou black tea at different fermentation degrees under industrial production conditions using flavor compound weighted network co-expression method

Article

作者: Yu, Zhi ; Ntezimana, Bernard ; Ni, Dejiang ; Chen, Yuqiong ; Zhu, Junyu ; Zhou, Jingtao ; Qin, Muxue ; Jiang, Xinfeng ; Zhang, De

Fermentation is a key process in Congou black tea, but there is limited research on the changes in flavor factors and their interrelationships during different fermentation stages under industrial production. This study applies sensory evaluation and metabolomics techniques to explore the interactions between flavors. Sensory evaluation indicated that the 4-h fermented sample exhibited the best overall performance. The experiment of adding aroma substances further revealed the significant effects of sweet aroma and green odor on taste of sweetness and astringency. Additionally, 532 flavor compounds were identified using high-resolution liquid chromatography-mass spectrometry and gas chromatography-mass spectrometry. Moreover, significant differences were observed in the volatile compounds derived from flavonoids, amino acids, and fatty acids of samples with different fermentation degrees. Furthermore, weighted co-expression network analysis of flavor compounds showed that the oxidation of polyphenols, especially catechins, plays an important regulatory role in content changes of volatile and other non-volatile compounds during fermentation.

2025-03-01·Reproductive Biology

Temporal optimization of meiotic arrest for enhancing oocyte maturity during in vitro maturation of porcine median antral follicles

Article

作者: Song, Beak ; Namkung, Ha Rin ; Han, Ji Won ; Lee, Seung Tae ; Jung, Su Bin ; Lee, Eun Song ; Nam, So Yeon

During in vitro maturation (IVM), median antral follicles (MAFs) were mechanically aspirated from the porcine ovarian cortex, and this process causes an early disconnection of follicular somatic cells from oocytes within antral follicles before the formation of graafian follicles. Thus, nuclear maturation is accelerated ahead of the completion of cytoplasmic maturation. Dibutyryl-cAMP (dbcAMP), a well-known cAMP modulator, is used to inhibit the resumption of meiosis in immature oocytes. However, there is no information on the optimal timeframe for sustaining meiotic arrest to enhance oocyte maturity during IVM. To determine the optimal duration of meiotic arrest, immature cumulus-oocyte complexes (COCs) from MAFs were cultured with 1 mM dbcAMP for 0, 4, 8, 12, 16, or 22 h, followed by further IVM without dbcAMP for 44, 40, 36, 32, 28, or 22 h. Subsequently, nuclear maturation, cumulus cell expansion score, perivitelline space size, glutathione (GSH) and reactive oxygen species (ROS) levels, and preimplantation development of parthenogenetic and in vitro-fertilized embryos were assessed in oocytes from each group. The results showed that a 16-h treatment with 1 mM dbcAMP within the 44-h IVM process yielded the highest oocyte maturity. Accordingly, we established an advanced IVM protocol for producing oocytes with superior maturity from porcine MAFs by achieving nuclear maturation 36 h after initiating IVM, using a 16-h treatment with 1 mM dbcAMP within the 44-h IVM process.

100 项与布拉地新钠相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01238	布拉地新钠	C01CE04	DB13242

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
褥疮	日本	Nipro Pharma Corp.	1993-01-19
皮肤溃疡	日本	Nipro Pharma Corp.	1993-01-19
心室功能不全	日本	Alfresa Pharma Corp.	1984-07-24

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASGCT2004	N/A	口腔肿瘤	-	Ganciclovir	獵憲醖範壓壓衊艱構顧(糧餘糧齋構網襯憲繭糧) = 顧鹽鏇遞鏇範獵簾網鬱築觸選網鏇壓憲獵選鬱 (獵夢蓋鹹選夢壓遞構遞 )	-	2004-05-01
				Dibutyryl-cAMP	觸選廠築鬱遞鹽衊願積(衊艱積窪網網夢範選繭) = 繭遞壓願願構襯鬱製築膚積醖餘夢願繭願糧齋 (積衊鑰觸鬱醖糧構糧鏇 )