Calcium Channel Ligand

S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca²⁺ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold.

(Rac)-PD0299685 is a Ca(2+) channel α2δ ligand that was investigated for relieving interstitial cystitis pain in a randomized, double-blind, placebo-controlled phase IIa study. (Rac)-PD0299685 demonstrated a clinically significant reduction in daily worst pain severity scores at the 60 mg dose compared to placebo. (Rac)-PD0299685 is also a potent voltage-dependent calcium channel inhibitor for the study of retina-related diseases.

PD-217014 is an α2δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity reactions. Its anti-allodynic effect is dose-dependent.

DMNPE-4 AM-caged-calcium, photolabile analogues of EGTA, is an extremely effective Ca²⁺ selective cage, with a K_d for Ca²⁺ of 48 nM and 19 nM at pH 7.2 and pH 7.4, respectively. DMNPE-4 AM-caged-calcium has a lower affinity for Ca²⁺ (K_d=~2 nM) after photolysis.

D-myo-Inositol-3,4,5-triphosphate hexasodium is an inositol (HY-B1411) derivative, a subtype-selective IP₃ receptor ligand, with K_d values of 31706 nM, 3019 nM and 11145 nM for rat type 1, type 2 and type 3 receptors, respectively.