cav3.1

SAK3 是一种新型的 nAChR 活性调节剂，可增强 T 型电压门控 Ca2+ 通道 (T-VGCC) 的活性，对 Cav3.1 和 Cav3.3 T 型 Ca2+ 通道电流均有增强作用。SAK3 对人神经母细胞瘤 SH-SY5Y 细胞中东莨菪碱诱导的胆碱能功能障碍有神经保护作用。SAK3 可用于研究记忆缺陷和阿尔茨海默病。

ACT-709478 is a potent, selective T-type calcium channel blocker that is orally active and capable of penetrating the brain. It is currently utilized in research focusing on generalized epilepsies[1].

5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50 = 0.54 μM), and Cav3.3 and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5(6)-EET is provided as a mixture of the free acid and lactone.

TTA-A2 是一种选择性 T 型钙通道拮抗剂，是一种有效的抗惊厥药，可减少孕烷 X 受体的激活。它对 Cav3.1 (a1G) 和 Cav3.2 (a1H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用，IC50 值分别为 89 和 92 nM。它可用于多种人类神经系统疾病的研究，包括睡眠障碍和癫痫。

T-Type calcium channel inhibitor 2 (compound 6g) 是一种 T 型钙通道的有效抑制剂，能够作用于 Cav3.1 (α1G) (IC50: 31.0 μM)、Cav3.2 (α1H) (IC50: 83.1 μM)、Cav3.3 (α1I) (α1H) (IC50: 69.3 μM)。T-Type calcium channel inhibitor 2 对 A549、HCT-116 细胞表现出细胞毒性，IC50s 分别为5.0、6.4 μM。

Cav 3.1 blocker 1 (compound 12) 作为一种 T 型钙通道 (T-type calcium channel) 阻滞剂，其对 Cav3.1 的抑制效果达到 IC50为160 nM。它对 Cav 3.2 的抑制作用较弱，IC50为5000 nM，对 Cav 3.3 和 Cav 1.2 则无抑制效果（IC50>10000 nM）。

ML218 是一种具有口服活性、选择性、高效性且可穿透血脑屏障的 T 型 Ca2+ 通道抑制剂（Cav3.2 和 Cav3.3 的 IC50 分别为 310 nM 和 270 nM）。ML218 可抑制丘脑下核（STN）神经元的突发性活动。

GTx1-15为一种抑制剂胱氨酸结 (ICK) 肽，能有效抑制电压依赖性钙通道 Cav3.1 以及电压依赖性钠通道 Nav1.3 和 Nav1.7。

TTA-P2 (T-Type calcium channel inhibitor) 是一种 T 型钙通道的有效抑制剂。TTA-P2 能够有效的穿透 CNS 并阻断小脑深部核神经元中的天然 T 型电流，完全消除野生型和突变型 Cav3.1 通道的窗口电流。TTA-P2 具有潜力进行神经疾病的研究。

Selective CaV3.1 channel blocker (IC50 values are 0.2 and 31.8 μM for hCaV3.1 and hCaV3.2 respectively). Also reversibly inhibits NaV1.8 and blocks KV2.1 channels.

ML218 hydrochloride is a selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor (Cav3.2 and Cav3.3 with IC50s of 310 nM and 270 nM , respectively).

Kurtoxin是一种选择性Cav3 (T-type) 电压门控Ca2+通道抑制剂，对Cav3.1 (α1G T-type) Ca2+通道的Kd值为15 nM。该化合物与中枢和外周神经元的L型、N型和P型Ca2+通道有高度亲和性，并对电压门控Na+通道也有交叉反应性。