voltage-gated ion channel

(R)-(+)-Bupivacaine hydrochloride 是一种电压门控钠通道 (sodium channel) 抑制剂，通过选择性阻断神经细胞膜上的电压门控钠离子通道，抑制钠离子内流，从而干扰神经冲动的产生与传导，实现局部麻醉效果。此化合物适用于急性疼痛的研究。

Photoswitchable Kv channel blocker (IC50 values are 2 and 64 μM at 500 nm and 380 nm respectively). Switches conformation from cis to trans at 500 nm and trans to cis at 380 nm. Exhibits minimal activity at Nav1.2 and L-type Ca2+ channels. Stimulates action potential firing of hippocampal neurons in vitro at 500 nm and restores visual responsiveness in blind mice at 380 nm. Fortin et al (2008) Photochemical control of endogenous ion channels and cellular excitability. Nat.Methods 5 331 PMID:18311146 |Polosukhina et al (2012) Photochemical restoration of visual responses in blind mice. Neuron 75 271 PMID:22841312 |Banghart et al (2009) Photochromic blockers of voltage-gated potassium channels. Angew.Chem.Int.Ed. 48 9097 PMID:19882609

Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported. CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.

DAD 是一种离子通道阻滞剂 (可阻断电压门控的钾离子通道)。DAD 也是一种对可见光作出响应的第三代光电开关。DAD 能够用于研究视觉功能。

DAD dichloride 是离子通道阻滞剂，能够阻断电压门控的钾离子通道 (potassium channels))。DAD dichloride 是一种对可见光作出响应的第三代光电开关。DAD dichloride 能够用于研究视觉功能。

μ-Conotoxin BuIIIB (Mu-Conotoxin BuIIIB) 是一种从Cone snails毒液中分离出的肽类分子，专门抑制哺乳动物神经元的电压门控钠通道 (VGSC)，以用作研究离子通道功能的生物探针。它在神经系统疾病（例如疼痛）的研究中具有潜在应用价值。

pan-HCN-IN-1 (Compound J&J12e) 作为HCN1离子通道的抑制剂，具有58 nM的IC50。在大鼠离体脑切片实验中，此化合物能够有效降低电压暂降响应，并且增强兴奋性突触后点位 (EPSP) 的累加效果。