数据质量标准
(1) 串联电阻 ≤ 20 MΩ;
(2) 封接电阻 ≥ 1 GΩ;
(3) 起始电流幅度适宜;
(4) 电流没有明显的自发性衰减(5分钟内自发性衰减小于5%);
(5) 在膜电位为-80mV下无明显的漏电流 (漏电流 ≤ 100 pA)。
数据分析
首先将每一个药物浓度作用后的电流和空白对照电流标准化(),然后计算每一个药物浓度对应的抑制率(1-)。对每一个浓度计算平均数和标准误, 并用以下的方程计算每种化合物的半抑制浓度:
用以上方程对剂量依赖效应进行非线性拟合, 其中c代表药物浓度,IC50为的半抑制浓度,h代表希尔系数。曲线拟合以及IC50的计算利用IGOR软件完成。
NaV1.1
Channel | Nav1.1 |
Gene | SCN1A |
Sources | human |
Catalog Ref. | ICE-CHO-Nav1.1 + β1 |
Expression system | CHO |
Method | whole cell patch clamp |
Reference inhibitor | TTX (5.6nM±0.8nM) |
Distribution | CNS and cardiac myocytes |
Related diseases | Pain, Epilepsy, Anxiety, Depression Related, Degenerative Diseases, Dravet syndrome, West syndrome, familial autism |
NaV1.2
Channel | NaV1.2 |
Gene | SCN2A |
Sources | human |
Catalog Ref. | ICE-HEK-Nav1.2 |
Expression system | HEK293 |
Method | whole cell patch clamp |
Reference inhibitor | TTX (11.7±0.783nM) |
Target | Pain, Seizure, Epilepsy, Anxiety, Depression Related, Degenerative Diseases |
NaV1.3
Channel | Nav1.3 |
Gene | SCN3A |
Catalog Ref. | ICE-HEK-Nav1.3 |
Sources | human |
Expression system | HEK293 |
Method | whole cell patch clamp |
Reference inhibitor | TTX (5.0±0.54nM) |
Target | Pain, Epilepsy, Anxiety, Depression Related |
NaV1.5
Channel | NaV1.5 |
Gene | SCN5A |
Catalog Ref. | ICE-HEK-Nav1.5 |
Sources | human |
Expression system | HEK293 |
Method | whole cell patch clamp |
Reference inhibitor | TTX (1.0μM± 438.7nM) |
Target | Brugada syndrome, long QT syndrome, progressive cardiac conduction disease ,dilated cardiomyopathy, sick sinus syndrome, and atrial fibrillation |
NaV1.6
Channel | Nav1.6 |
Gene | SCN8A |
Catalog Ref. | ICE-HEK-Nav1.6 |
Sources | human |
Expression system | HEK293 |
Method | whole cell patch clamp |
Reference inhibitor | TTX (1.9±0.302nM) |
Target | Epilepsy, Degenerative Diseases, |
NaV1.7
Channel | Nav1.7 |
Gene | SCN9A |
Catalog Ref. | ICE-HEK-Nav1.7 |
Sources | human |
Expression system | HEK293 |
Method | whole cell patch clamp |
Reference inhibitor | TTX (1.3±0.508nM) |
Target | Pain, Anxiety, Depression Related, erythromelalgia |
NaV1.8
Channel | NaV1.8 |
Gene | SCN10A |
Catalog Ref. | ICE-HEK-Nav1.8 |
Sources | human |
Expression system | HEK293 |
Method | whole cell patch clamp |
Reference inhibitor | TTX (2.90±0.803nM) |
Target | Pain, Anxiety, Depression Related |