sarcoplasmic

Tetracaine hydrochloride (Amethocalne HCl) (Pontocaine), a potent local anaesthetic, is a channel function allosteric inhibitor. It is primarily used as an antipruritic and topically in ophthalmology, and it has been used for surface and spinal anesthesia.

Thapsigargin is a natural product, an inhibitor of sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

JTV-519 Formate is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA). JTV-519 Formate is also a partial agonist of ryanodine receptors in striated muscle. JTV-519 Formate exhibits antiarrhythmic and cardioprotective properties.

JTV-519 is a Ca2+-dependent blocker and prevents abnormal Ca(2+) leak from the sarcoplasmic reticulum in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors.

Caldaret HCl is an intracellular Ca2+ modulator that regulates calcium homeostasis at the sarcoplasmic reticulum and cell membrane, and can be used to study acute myocardial infarction and heart failure.

Praziquantel (Droncit) increases the permeability of the tegument of susceptible worms, resulting in an influx and increase in intra-tegumental calcium leading to rapid contractions and paralysis of the worm's musculature through a subsequent increase in levels of calcium in the sarcoplasmic reticulum. Praziquantel is a pyrazinoisoquinoline derivative with anthelminthic property. In addition, vacuolization of the tegumental syncytium and blebbing results in tegument disintegration, leads to antigen exposure and elicit host defense responses to the worm.

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1 and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. Dantrolene sodium hemiheptahydrate (Sodium dantrolene) is the sodium salt form of dantrolene, a hydantoin derivative, and direct-acting skeletal muscle relaxant.

Dantrolene is a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.

JTV-519 free base (K201 free base), known for its antiarrhythmic and cardioprotective properties, acts as a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and as a partial agonist of ryanodine receptors in striated muscle.

JTV-519 hemifumarate,Antiarrhythmic and cardioprotective properties. is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle.

Paxilline is an indole alkaloid mycotoxin from *Penicillium paxilli*, acting as a potent BK channel inhibitor via an almost exclusively closed-channel block mechanism. Paxilline possesses significant anticonvulsant activity.

Annonacin is an acetogenin that promotes cytotoxicity by inhibiting the mitochondrial complex and acts as the active agent in Graviola leaf extract, inhibiting sodium potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pumps[1].

Istaroxime hydrochloride (PST2744 hydrochloride) is a Na+ K+-ATPase inhibitor and sarcoplasmic endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator, a novel positive inotropic compound that can be used to study acute heart failure.

SERCA2a activator 1 is a sarco endoplasmic reticulum Ca2+-dependent ATPase 2a activator. SERCA2a activator 1 decreases phospholamban inhibition and enhances the systolic and diastolic functions of the heart.

Xestospongin C ((-)-Xestospongin C) is a selective inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor and also inhibits sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA). It has neuroprotective effects in APP PS1 AD mice, improving cognitive and pathological deficits associated with Alzheimer's disease.

3',4'-Dichlorobenzamil HCl is an inhibitor of Na+ transport, Na+/Ca2+ exchanger, sarcoplasmic reticulum Ca2+ release channels.

BK 129 is a local anesthetic with relaxant properties. BK 129 inhibits Ca2+ entry into the smooth muscle cell and Ca2+ release from sarcoplasmic reticulum.

JTV-519 fumarate (K201 fumarate) is a SERCA blocker and partial agonist at the ryanodine receptor with antiarrhythmic and cardioprotective effects, improves sarcoplasmic reticulum calcium leakage, and may be useful in the study of anxiety disorders.

Atosiban (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

L594881, also known as 3',4'-Dichlorobenzamil or DCB, is an inhibitor of Na+ Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels. L594881 can inhibit Na+ Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels.

Azumolene sodium dihydrate is a muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum. Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor.

Istaroxime, also known as PST-2744, is a positive inotropic agent that mediates its action through inhibition of sodium potassium adenosine triphosphatase (Na+ K+ ATPase). Na+ K+ ATPase inhibition increases intracellular sodium levels, which reverses the driving force of the sodium calcium exchanger, inhibiting calcium extrusion and possibly facilitating calcium entry. Additionally, Istaroxime increases intracellular calcium by improving the efficacy by which intracellular calcium triggers sarcoplasmic reticulum calcium release, and by accelerating the inactivation state of L-type calcium channels, which allow for calcium influx.

Azumolene sodium anhydrous is a muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum. Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor. Azumolene, an equipotent dantrolene analog, inhibits a component of SOCE coupled to activation of RyR1 by caffeine and ryanodine, whereas the SOCE component induced by thapsigargin is not affected.