diastolic

Strophanthidin (Strophanthidine) 是黄花夹竹桃中的一种类固醇，可增加舒张期和收缩期胞内 Ca2+浓度。它在 0.1 和 1 nmol L 增加Na+ K+-ATPase 活性，1到100 μ mol L 抑制Na+ K+-ATPase 活性，10 和 100 nmol L 对Na+ K+-ATPase 活性无影响。

SERCA2a activator 1 是一种肌肉 内质网 Ca2+ 依赖性 ATPase 2a 激活剂。 SERCA2a activator 1 降低受磷蛋白抑制并增强心脏的收缩和舒张功能。

Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。

Ivabradine hydrochloride (S 16257-2) 是一种可口服的，超极化激活的环核苷酸门控离子通道通道阻滞剂。

Alagebrium chloride (ALT711) 是晚期糖基化终产物(AGE) 抑制剂。

RO 363 is an effective inotropic stimulant and is a cardiovascular modulator that decreases diastolic blood pressure and pronounces increases in myocardial contractility. Ro 363 is an effective and highly selective β1-adrenoceptor agonist.

O-Desmethylcarvedilol (Desmethylcarvedilol) 是 Carvedilol 的活性代谢物，为一种非选择性 β-肾上腺素受体 (β-AR) 拮抗剂。该化合物能够抑制在表达瑞安诺丁受体 2 (RyR2) R4496C 突变的 HEK293 细胞中由储存超载所引发的钙释放，其 IC50 为 7.62 µM。此外，O-Desmethylcarvedilol 可以在清醒兔子中减缓心率上升，并预防 Isoproterenol 诱导的舒张压下降，ED50 分别为 32 和 5 µg kg。

Esmolol acid (ASL-8123) hydrochloride 是一种弱效的β-肾上腺素能受体拮抗剂。Esmolol acid hydrochloride 能以剂量依赖的方式抑制 Isoproterenol 诱导的心率及舒张压变化，可用于肾衰竭的相关研究。

A-80b is a synthesized pyridazino[4,5-b]indole derivate with potent and long-lasting antihypertensive activity. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. A-8

C2 Ceramide (d14:1 2:0) is a bioactive sphingolipid. Dietary administration of C2 ceramide (d14:1 2:0) (100 μM) induces lipotoxic cardiomyopathy via increasing diastolic and systolic diameter as well as reducing fractional shortening and the number of normal cardiac contractile events in Drosophila.

Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties.1,2 It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM).1 Quazinone (10-300 μg kg) increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner, as well as decreases systolic and diastolic blood pressure.2 It also inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smooth muscle cells in a concentration-dependent manner.3

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2 |1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): Role of the alpha-1L adrenoceptor in tissue selectivity, part II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997).

Alinidine hydrobromide, a specific bradycardic agent, diminishes the slope of the diastolic depolarization in sinoatrial tissue and Purkinje fibers [1].

Ro 363 hydrochloride 是一种有效的，高度选择性的 β1 肾上腺素受体 (β1-adrenoceptor) 激动剂。Ro 363 hydrochloride 是有效的正性肌力活化剂。Ro 363 hydrochloride 是心血管调节剂，可降低舒张压，显著增加心肌收缩力。

Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-​1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.)​. Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mitochondrial fission, and improved right ventricular diastolic dysfunction during IR injury.

Zofenoprilat是一种血管紧张素转换酶(ACE; IC50 = 8 nM for the rabbit lung enzyme)的抑制剂，同时也是前体药zofenopril的活性代谢产物。它能够抑制分离的豚鼠小肠中由血管紧张素I或缓激肽诱导的收缩(EC50s = 3 and 1 nM, respectively)。在人类脐静脉内皮细胞(HUVECs)中，Zofenoprilat (10 nM)降低基础内皮素-1分泌和一氧化氮(NO)生成，并阻止TNF-α诱导的活性氧种(ROS)增加以及谷胱甘肽(GSH)水平降低。Zofenoprilat (10 µM)保护初级人类心脏微血管内皮细胞免受多柔比星诱导的细胞毒性。此外，Zofenoprilat (10 µM)还能增加HUVECs中的硫化氢(H2S)生成，以及细胞的黏着、迁移和增殖。在以400 µM浓度使用时，它可以减少Langendorff分离的大鼠心脏灌流缺血再灌注损伤模型中的舒张末压和乳酸脱氢酶(LDH)释放。

ent-(+)-verticilide is an effective and specific inhibitor of cardiac ryanodine receptor (RyR2) calcium release channels, demonstrating antiarrhythmic properties. It suppresses RyR2-mediated diastolic Ca2+ leak and shows greater potency and a unique action mechanism compared to Dantrolene and Tetracaine. ent-(+)-verticilide serves as a valuable tool for exploring the therapeutic potential of addressing RyR2 hyperactivity in cardiac and neurological conditions [1].

RG100204, 作为一种具备口服活性的AQP9抑制剂，它表现出显著的抗炎效果。该化合物能够缓解由脓毒症引发的心脏功能障碍（收缩与舒张功能），优化肾功能，并有效减少细胞损伤指标LDH的升高。

SVC-02,作为一种血管抑制素 (vasohibin (VASH)) 抑制剂,具有11 nM的IC50值.该化合物能减少微管蛋白的去酪氨酸化过程,并显示出在改善射血分数保留心力衰竭 (HFpEF) 时降低心肌僵硬性的研究潜力.

Oblongine chloride may have potential haemodynamic effects, it can cause a dose-dependent reduction of systolic and diastolic blood pressure, and that these effects are not mediated by α²-adrenergic receptor stimulation.

Dysolenticin J shows significant vasodilative effects on intact rat aortic rings with a diastolic degree of 87.4% at 10 ug mL.

Serpinin 作为蛋白酶抑制剂 Nexin-1 (PN-1) 的激动剂，通过 cAMP-PKA-Sp1 信号通路增强 PN-1 的表达，并促进内分泌细胞的颗粒生成。此外，Serpinin 亦作为β-肾上腺素能受体的选择性激动剂，通过与 β1-肾上腺素能受体的相互作用激活 AC-cAMP-PKA 途径，从而调控心肌的收缩与舒张。其衍生物 pGlu-serpinin 通过上调 Bcl2 mRNA 的转录具有神经保护功能，常用于研究分泌功能的调节。

Chitoheptaose 是一种壳八糖，从螃蟹、虾和龙虾等甲壳类动物的外骨骼中提取。Chitoheptaose 具有抗氧化、抗炎和抗凋亡活性，常用于心肌炎研究，展现出心脏保护作用。其在改善心脏参数（左心室内部尺寸、收缩末期和舒张末期、射血分数和缩短分数）以及抑制炎症细胞因子 (IL-1β) 方面表现突出。