更新于：2024-11-01

AC x β-adrenoceptors

更新于：2024-11-01

基本信息

关联

项与 AC x β-adrenoceptors 相关的药物

Colforsin Daropate Hydrochloride

考福新达普酸盐酸盐

靶点

AC x β-adrenoceptors

作用机制

AC刺激剂 [+1]

在研机构

Nippon Kayaku Co., Ltd.

原研机构

Nippon Kayaku Co., Ltd.

在研适应症

心脏衰竭

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

日本

首次获批日期1998-10-16

100 项与 AC x β-adrenoceptors 相关的临床结果

登录后查看更多信息

100 项与 AC x β-adrenoceptors 相关的转化医学

登录后查看更多信息

0 项与 AC x β-adrenoceptors 相关的专利（医药）

登录后查看更多信息

1,793

项与 AC x β-adrenoceptors 相关的文献（医药）

2024-09-19·Current Cardiology Reviews

Importance of Zinc Homeostasis for Normal Cardiac Rhythm

Article

作者: Hejazi, Seyedeh Fatemeh ; Mollazadeh, Reza ; Kokhabi, Pejman ; Pazoki-Toroudi, Hamidreza ; Hossein Nezhad, Aida

<p>Current arrhythmia therapies such as ion channel blockers, catheter ablation, or implantable cardioverter defibrillators have limitations and side effects, and given the proarrhythmic risk associated with conventional, ion channel-targeted anti-arrhythmic drug therapies, a new approach to arrhythmias may be warranted. Measuring and adjusting the level of particular ions that impact heart rhythm can be a simple and low-complication strategy for preventing or treating specific arrhythmias. In addition, new medicines targeting these ions may effectively treat arrhythmias. Numerous studies have shown that intracellular and extracellular zinc concentrations impact the heart's electrical activity. Zinc has been observed to affect cardiac rhythm through a range of mechanisms. These mechanisms encompass the modulation of sodium, calcium, and potassium ion channels, as well as the influence on beta-adrenergic receptors and the enzyme adenylate cyclase. </p><p> Moreover, zinc can either counteract or induce oxidative stress, hinder calmodulin or the enzyme Ca (2+)/calmodulin-dependent protein kinase II (CaMKII), regulate cellular ATP levels, affect the processes of aging and autophagy, influence calcium ryanodine receptors, and control cellular inflammation. Additionally, zinc has been implicated in the modulation of circadian rhythm. Additionally, zinc has been implicated in the modulation of circadian rhythm. In all the above cases, the effect of zinc largely depends on the normal or increased cellular level of zinc, which shows the importance of maintaining the serum and intracellular levels of zinc within the normal range.</p>

2024-09-01·Hypertension Research

Mechanistic study on vasodilatory and antihypertensive effects of hesperetin: ex vivo and in vivo approaches

Article

作者: Yan, Chong Seng ; Wei, Xu ; Tan, Chu Shan ; Loh, Hui Wei ; Wen, Xu ; Wang, Xuye ; Yam, Mun Fei ; Tew, Wan Yin

Hesperetin is one of the prominent flavonoids found in citrus fruit. Several research studies have reported that hesperetin can promote vasodilation in vascular tissue by increasing the level of nitric oxide and cyclic nucleotides. However, these may not be the only pathway for hesperetin to exert its vasodilatory effect. In addition to vasodilation, hesperetin has been found to carry an antihypertensive effect through intraperitoneal injection, although no study has comprehensively investigated the antihypertensive effect of hesperetin through oral administration. Therefore, this study aimed to determine the possible mechanism pathways involved in hesperetin-induced vasodilation and investigated its antihypertensive effects on hypertensive rats' model via oral administration. The ex vivo experimental findings showed that the NO/sGC/cGMP signalling pathway was involved in hesperetin-mediated vasodilation. Moreover, hesperetin activated the AC/cAMP/PKA pathway through PGI₂ and activated the β₂-adrenergic receptor. Hesperetin can act as a voltage-gated potassium channel (K_V) and ATP-sensitive potassium channel (K_ATP) opener. The intracellular calcium in vascular smooth muscle was reduced by hesperetin through blocking the voltage-operated calcium channels (VOCC) and inositol triphosphate receptor (IP₃R). In the in vivo assessment, hesperetin shows a significant decrease in Spontaneously Hypertensive rats' blood pressure following 21 days of oral treatment. The sub-chronic toxicity assessment demonstrated that hesperetin exhibited no deleterious effects on the body weights, clinical biochemistry and haematological profile of Sprague-Dawley rats. This study implies that hesperetin holds promise as a potential medication for hypertension treatment, devoid of undesirable side effects.

2024-06-01·Naunyn-Schmiedeberg's Archives of Pharmacology

New phosphodiesterase-4 inhibitors present airways relaxant activity in a guinea pig acute asthma model

Article

作者: Vasconcelos, Luiz Henrique César ; Silva, Maria da Conceição Correia ; Silva, Bagnólia Araújo da ; Martins, Italo Rossi Roseno ; Queiroga, Fernando Ramos ; da Silva, Patricia Mirella ; Cavalcante-Silva, Luiz Henrique Agra ; de Melo Medeiros, Millena ; Lima, Lidia Moreira ; da Costa Nunes, Isabelle Karine

Asthma is a disease characterized by chronic inflammation and hyper responsiveness of airways. We aimed to assess the relaxant potential of phosphodiesterase-4 (PDE4) inhibitors N-sulfonilhidrazonic derivatives on non-asthmatic and asthmatic guinea pig trachea. Firstly, guinea pigs were sensitized and challenged with ovalbumin, and then morphological, and contractile changes were evaluated resulting from asthma, followed by evaluation of relaxant effect of derivatives on guinea pig trachea and the cAMP levels measurement by ELISA. It has been evidenced hypertrophy of airway smooth muscle, inflammatory infiltrate, and vascular abnormalities. Moreover, only sensitized tracheal rings were responsive to OVA. Contractile response to histamine, but not to carbachol, was greater in sensitized animals, however the relaxant response to aminophylline and isoprenaline were the same in non-asthmatics and asthmatics. N-sulfonilhidrazonic derivatives presented equipotent relaxant action independent of epithelium, with exception of LASSBio-1850 that presented a low efficacy (< 50%) and LASSBio-1847 with a 4-fold higher potency on asthmatics. LASSBio-1847 relaxant curve was impaired in the presence of propranolol and potentiated by isoprenaline in both groups. Furthermore, relaxation was potentiated 54- and 4-fold by forskolin in non-asthmatics and asthmatics, respectively. Likewise, LASSBio-1847 potentiated relaxant curve of aminophylline 147- and 4-fold in both groups. The PKA inhibitor H-89 impaired the relaxant potency of the derivative. Finally, LASSBio-1847 increased tracheal intracellular cAMP levels similarly to rolipram, selective PDE4 inhibitor, in both animals. LASSBio-1847 showed to be promising to relax guinea pig trachea from non-sensitized and sensitized guinea pigs by activation of β₂-adrenergic receptors/AC/cAMP pathway.