ryanodine receptor 1

Dantrolene sodium (Dantrolene sodium salt) is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.

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.

Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It raises cytosolic calcium levels through Ryanodine receptor-mediated release from the endoplasmic reticulum and facilitates extracellular influx via TRPM2 channels [1][2][3].

Paraxanthine (1,7-dimethylxanthine) is a metabolite of caffeine (sc-202514) which functions as an adenosine receptor ligand and a PARP-1 inhibitor in pulmonary epithelial cells. Studies suggest that Paraxanthine is structurally similar to caffeine and possibly mediates the physiological effects of caffeine. Also Paraxanthine acts as a competitive phosphodiesterase inhibitor, which increases intracellular cAMP, activates PKA, inhibits TNF-α and leukotriene synthesis. In addition, Paraxanthine acts as a Na+ K+ ATPase enzymatic effector.

RyRs activator 3 (compound A4) serves as an insecticide highly effective against both the diamondback moths, M. separata and P. xylostella, exhibiting an LC50 of 3.27 mg L for controlling diamondback moth populations. The mechanism of action involves binding to the ryanodine receptor, which elevates cytoplasmic Ca2+ concentration, resulting in biological toxicity [1].

Maurocalcine is a cell-permeable agonist for ryanodine receptor (RyR) subtypes 1, 2, and 3. It enhances [3 H]ryanodine binding to RyR1 with an EC50 of 2558 nM and demonstrates an apparent affinity for RyR2 at 14 nM. This compound is suitable for in vivo cell tracking and other cellular imaging applications [1] [2] [3].

TMDJ-035 is a selective inhibitor of the RyR2 (ryanodine receptor 2). It effectively suppresses abnormal calcium (Ca^2+) waves and transients in isolated cardiomyocytes derived from mice with RyR2 mutations. As such, TMDJ-035 serves as a valuable tool in research for elucidating the gating mechanisms and dynamics of the RyR2 channel [1].

Compound B18 (RyRs activator 4) is an insect ryanodine receptor activator that exhibits larvicidal activity against Mythimna separata with an LC50 value of 1.32 mg L [1].

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].

Maurocalcine TFA acts as an agonist for ryanodine receptor (RyR) channels 1, 2, and 3, demonstrating cell-penetrating capabilities. It induces binding of [3H]ryanodine to RyR1 with an EC50 of 2558 nM and exhibits an apparent affinity of 14 nM for RyR2. This compound is applicable for in vivo cell tracking or other cellular imaging techniques.