contractility

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Tetraethylammonium chloride is a quaternary ammonium compound. It is a non-selective potassium channel blocker. It is a good substrate for organic cation transporter proteins and has antitumor properties.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

Silperisone HCl (RGH-5002) blocks sodium and calcium channels in cells, decreases excitability and contractility of muscle cells, reduces peripheral tone, and acts as a muscle relaxant and peripheral vasodilator. Silperisone HCl is used to treat recurrent painful myoclonus due to spinal cord injury, abnormal hypertonia due to cerebrovascular disease, dystonia symptoms, cone tension syndrome, multiple sclerosis myospasm and myelitis. silperisone is a sodium channel protein type 2 alpha channel blocker. silperisone is an organosilicon similar to tolperisone, an organosilicon compound with centrally acting muscle relaxant properties.

Pseudoginsenoside RT1, isolated from the fruit of Randia siamensis, exhibits acute ichthyotoxic activity and can cause a decrease in blood pressure, an increase in heart rate, and heightened spontaneous contractility of the uterus.

1. Praeruptorin C and E can relax swine coronary artery and decrease contractility in guinea-pig left atria, these effects are similar in many respects to those displayed by drugs that have calcium entry blocking activity. 2. Praeruptorin D and E can prot

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

13-Hydroxylupanine, a characteristic alkaloid of sweet lupins, inhibits ganglionic transmission, reduces cardiac contractility, and induces contraction of uterine smooth muscle [1].

APJ Receptor Agonist 8 (compound 99) acts as an agonist for the APJ receptor and enhances load-independent cardiac contractility in isolated perfused rat hearts [1].

ORM-3819 is a potent and selective PDE III inhibitor. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization.

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.

Acotiamide hydrochloride is a selective, orally active, reversible acetylcholine ester (AChE) inhibitor (IC50: 1.79 μM) that increases gastric contractility, accelerates delayed gastric emptying, and can be used to study functional dyspepsia and intestinal inflammation in gastric motility disorders.

Neuropeptide Y (NPY), a neuropeptide, plays roles in regulating appetite, vasoconstriction, cardiac contractility, and intestinal secretion, acting as an agonist for NPY receptors Y1, Y2, and Y5. Expressed ubiquitously, NPY modulates cellular responses by selectively inhibiting forskolin-induced cAMP accumulation in L-M(TK-) cells expressing rat Y1 or Y2 and in HEK293 cells expressing rat Y5, more so than in cells expressing rat Y4 receptors (EC50s = 0.15, 2.7, 0.66, and >1,000 nM, respectively). Additionally, it elevates perfusion pressure in isolated guinea pig hearts (EC30 = 1.3 nM) and, when administered intracerebroventricularly at 300 pmol/animal, it notably increases food intake in rats.

(Phe2,Orn8)-Oxytocin, a selective V1 vasopressin agonist, exhibits sustained contractility in rabbit epididymis, achieving an EC50 value of 280 nM [1].

(Phe2,Orn8)-Oxytocin acetate, a selective V1 vasopressin agonist, demonstrates pronounced contractility induction in rabbit epididymis, characterized by a sustained response with an EC50 value of 280 nM [1].

PD 122860 is a dihydropyridine with calcium channel blocking and sodium channel stimulating properties. In the rat heart, PD 122860 increased left ventricular contractility, decreased coronary resistance and altered the shape of the electrocardiogram T-wa

Pyrromecaine is a local anesthetic used for surface anesthesia. Pyromecaine has a wide spectrum of antiarrhythmic action, exerts a favorable effect on the contractility of the left ventricle, and on the myocardial blood flow following the ligation of the

Ro 363 hydrochloride is an effective, highly selective agonist of β 1-adrenoceptor. Ro 363 hydrochloride is an effective inotropic stimulant. Ro 363 hydrochloride is a cardiovascular regulator, which can reduce diastolic blood pressure and significantly increase myocardial contractility.

CK-963 is an activator of cardiac troponin (cTnC) with a K i of 11.5 μM, exhibiting activity in enhancing cardiac contractility in Sprague-Dawley rats [1].

GLX481304 is a selective Nox-2 and Nox-4 inhibitor, exhibiting IC50 values of 1.25 μM. It inhibits ROS production in isolated mouse cardiomyocytes and enhances their contractility. This compound is useful in research focused on ischemic cardiac injury [1].

GSK1702934A, a selective TRPC3 agonist, modulates cardiac contractility and arrhythmogenesis through TRPC3 activation.

Disopyramide HCl is the salt form of Disopyramide, an antiarrhythmic medication used in the treatment of ventricular tachycardia. It is a sodium channel blocker and therefore classified as a Class 1a anti-arrhythmic agent. Disopyramide has a negative inotropic effect on the ventricular myocardium, significantly decreasing the contractility. Disopyramide also has an anticholinergic effect on the heart which accounts for many adverse side effects. Disopyramide is available in both oral and intravenous forms, and has a low degree of toxicity.

BBR 2160 is a dihydropyridine derivative belonging to the group of the so-called tiampidine. BBR 2160 has calcium-antagonistic properties in cardiac tissue. Intracellular microelectrodes have been used to characterize the electrophysiological properties o

ATI-22-107 is a positive cardiac inotropic agent which may affect myocyte calcium cycling and contractility.

OR-1855 is an active Levosimendan metabolite, has effect on human myometrial contractility.

Acotiamide is an orally active, selective, and reversible acetylcholinesterase (AChE) inhibitor with an IC50 of 1.79 μM. It is a gastroprokinetic agent that enhances gastric contractility and accelerates delayed gastric emptying, with potential for research in functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory [1] [2] [3].

CCG-271423 is a potent and selective inhibitor of GRK5, demonstrating activity against GRK5 (IC50: 0.0021 μM) and GRK2 (IC50: 44 μM); it reduces Ca2+ transients and inhibits cardiomyocyte contractility.

GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1]. [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.

Disopyramide, a sodium channel blocker in the Class of 1a anti-arrhythmic agent, is used in the treatment of Ventricular Tachycardia. Disopyramide has a negative inotropic effect on the ventricular myocardium, resulting in a significant decrease in contra

TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility.

Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1 receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.

VU590 is a potent and moderately selective inhibitor of extrarenal medullary potassium ROMK (Kir1.1) that also inhibits Kir7.1 and modulates uterine myometrial contractility and melanocortin signalling.

Cibenzoline is an antiarrhythmic agent that inhibits the KATP channel by directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline shows little anticholinergic activity. Cibenzoline markedly reduces LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for hypertrophic obstructive cardiomyopathy research[1][2].

Levosimendan (OR1259) is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner.

R 59-022 (DKGI-I) is a diacylglycerol kinase (DGK) inhibitor and a 5-HT Receptor antagonist that blocks filovirus internalization in host cells. R 59-022 activates protein kinase C (PKC), inhibits intestinal smooth muscle contractility, and enhances O2- production induced by 1-oleoyl-2-acetylglycerol.