Membrane Transporters/Ion Channels
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TRPV4 blocker
GSK2193874被确定为选择性的口服活性TRPV4阻滞剂,可通过重组TRPV4通道和天然内皮TRPV4电流抑制Ca(2+)流入。
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TRPA1 channel blocker
A 967079是选择性TRPA1通道阻滞剂(人和大鼠TRPA1受体的IC50值分别为67和289 nM)。
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- L Jin, .et al. Acrolein but not its metabolite, 3-Hydroxypropylmercapturic acid (3HPMA), activates vascular transient receptor potential Ankyrin-1 (TRPA1): Physiological to toxicological implications, Toxicol Appl Pharmacol, 2021, Jul 13;426:115647 PMID: 34271065
- L. Jin, .et al. Crotonaldehyde-induced vascular relaxation and toxicity: Role of endothelium and transient receptor potential ankyrin-1 (TRPA1), Toxicology and Applied Pharmacology, 2020, 398(1),
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TRPA1 activatior/TRPM8 blocker
Cannabichromene是一种主要的非精神植物大麻素,可抑制内源性大麻素失活并激活瞬时受体电位锚蛋白1(TRPA1)。内源性大麻素和TRPA1均可调节肠胃蠕动。
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TRPA1 channel blocker
TCS 5861528是TRPA1通道阻滞剂和AITC和4-HNE诱发的钙流入的拮抗剂。
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AMPA Receptor Blocker
IEM 1754 Dihydrobromide是AMPA受体的电压依赖性明渠阻断剂。
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chloride channel blocker
NPPB是一种氯离子通道阻滞剂(IC50 = 80 nM),也被确定为GPR35激动剂。
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CaCC blocker
Talniflumate是一种钙激活的氯离子通道(CaCC)(hCLCA1/mCLCA3)阻滞剂;在细胞培养和动物模型中减少粘蛋白的合成和释放。
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K+ channel blocker?
E-4031 dihydrochloride是KV11.1(hERG)通道的选择性阻滞剂;禁止快速延迟整流器K+电流(IKr)。
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IKs blocker
JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
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Potassium channel blocker
Cesium chloride是钾通道阻滞剂。抑制起搏器电流(If)和超极化激活的阳离子电流(Ih)。通过灭活GSK-3β来防止血清和钾缺乏的小脑颗粒神经元中caspase-3的激活和神经元凋亡。
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potassium-competitive acid Blocker
TAK-438 (vonoprazan)是一种新型的钾竞争酸阻滞剂。
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Potassium channel blocker
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk.
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Kv1.3 blocker
PAP-1 (5-(4-Phenoxybutoxy)psoralen) 是一种有效的,选择性的,口服活性的?Kv1.3?阻滞剂 (EC50=2 nM)。PAP-1 以使用依赖性方式阻止 Kv1.3,并通过优先绑定到通道的 C 型灭活状态来起作用。
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- Samuel Drinkall, .et al. The two pore potassium channel THIK-1 regulates NLRP3 inflammasome activation, Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
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Kir7.1 potassium channels blocker
ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
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Potassium Channel Blocker
TRAM-34是中等电导Ca2+激活的K+通道(KCa3.1)(Kd = 20 nM)的高度选择性阻滞剂。在KV,BKCa,KCa2,Na+,CRAC和Cl-通道上具有200-1500倍的选择性。抑制有丝分裂刺激对淋巴细胞的激活。
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- Samuel Drinkall, .et al. The two pore potassium channel THIK-1 regulates NLRP3 inflammasome activation, Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
- Cheong Hoon Seo, .et al. Altered K Ca 3.1 expression following burn injury and the therapeutic potential of TRAM-34 in post-burn hypertrophic scar formation, Transl Res, 2021, Apr 24 PMID: 33905948
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Na+ channel blocker
Amiloride HCl是一种Na+通道阻滞剂,还抑制TRPP3通道和Na+/H+交换剂(NHE)。
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- Yu Y, .et al. Expression, Localization and Functional Activity of the Major Na+/H+ Exchange Isoforms Expressed in the Intestinal Cell Line Caco-2BBe, Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thomas D. Williams, .et al. The physiological regulation of macropinocytosis during Dictyostelium growth and development, J Cell Sci, 2018, Mar 15; 131(6): jcs213736 PMID: 29440238
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Sodium channel blocker/DNMT 抑制剂
Procainamide HCl是钠通道阻滞剂,又是DNA甲基转移酶抑制剂。
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Sodium channel blocker
Encainide hydrochloride是一种钠通道阻滞剂,具有Ic类抗心律不齐的作用。Encainide是一种非手性抗心律失常药和苯甲酰苯胺衍生物。
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Cardiac Na+ channel blocker
Flecainide acetate是1C类抗心律不齐药物,特别用于室上性心律失常的治疗;通过阻断心脏中的Nav1.5钠通道起作用,从而延长了心脏动作电位。
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Sodium channel Blocker
A 803467是NaV1.8通道的选择性阻滞剂(hNaV1.8,hNaV1.3,hNaV1.7,hNaV1.5和hNaV1.2通道的IC50值分别为8、2450、6740、7340和7380 nM)。
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Sodium channel blocker
Raxatrigine (GSK1014802)是一种新型的钠通道阻滞剂,是一种有效的抗惊厥药物。在大鼠中,GSK1014802(20-80 mg/kg p.o.)以剂量依赖的方式减轻了苯环利定(PCP)诱导的逆向学习障碍,这表明GSK1014802在治疗精神分裂症的认知潜力方面具有潜力。 GSK2还是人MAO-B的有效抑制剂,pIC50值为7.96,但不抑制人MAO-A。
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Ion channel blocker
Vernakalant hydrochloride是一种研究性混合离子通道阻滞剂,可以以2至5 mg/kg的剂量终止人的急性心房纤颤(AF),并且与现有药物相比,对房颤的选择性更高。在抗心律不齐的治疗中。
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- Joe Z.Zhang, .et al. A Human iPSC Double-Reporter System Enables Purification of Cardiac Lineage Subpopulations with Distinct Function and Drug Response Profiles, Cell Stem Cell, 2019, 24, 1-10
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Sodium Channel Blocker
Pilsicainide是一种水溶性的选择性Na+通道阻滞剂。
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NMDA receptor 拮抗剂
Orphenadrine柠檬酸盐是NMDA受体拮抗剂,Ki为6.0μM,还是HERG钾离子通道阻断剂。
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Na+ channel blocker
Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
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Sodium channel Blocker
QX 314 chloride是利多卡因的膜不可渗透的季衍生物,一种电压激活的Na+通道阻滞剂。
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Sodium channel blocker
Disopyramide是一种抗心律不齐药物(IA类)和钠通道阻滞剂。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Sodium channel blocker
Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.
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Calcium channel blocker
NNC 55-0396是Mibefradil衍生物,是一种高度选择性的T型钙通道阻滞剂;分别在INS-1细胞中抑制Cav3.1 T型通道和HVA电流的IC50值为6.8和> 100μM。
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Calcium channel blocker
Mibefradil dihydrochloride是钙通道阻滞剂,对T型Ca2+通道具有中等选择性,对T型和L型通道的IC50值分别为2.7 uM和18.6 uM。
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calcium channel blocker
Azelnidipine是一种钙阻断剂,可减轻肝纤维化并可能增加抗氧化防御能力。可以减轻肝纤维化并可能增加抗氧化防御能力。
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L-type calcium channel blocker.
Nifedipine是一种L型钙通道阻滞剂。
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Calcium channel blocker
(S)-Amlodipine是氨氯地平的(S)-对映体,具有活性的二氢吡啶钙通道阻滞剂主要存在于(-)-异构体中。
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Calcium channel blocker
Cilnidipine是提供血管平滑肌中L型电压门控钙通道和交感神经末梢N型钙通道的双重阻滞剂。
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calcium channel blocker
Cinnarizine是哌嗪的药物衍生物,其特征在于抗组胺药和钙通道阻滞剂。
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calcium channel blocker
Nilvadipine (ARC029)是一种钙通道阻滞剂(CCB),用于治疗高血压和慢性主要脑动脉阻塞。
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N-type calcium channel blocker
NP118809是有效的N型钙通道阻滞剂(IC50 = 0.11 uM);对L型钙通道的选择性好。
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L-type calcium channel blocker
Amlodipine是一种L型钙通道阻滞剂,具有降压作用。它抑制去极化大鼠主动脉中Ca2 +诱导的收缩(IC50 = 1.9 nM),并在心血管疾病中显示出血管保护作用。
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K(Ca) 3.1 channel blocker
NS6180是一种新型有效的选择性KCa3.1通道抑制剂(IC50 = 9 nM),可防止T细胞活化和炎症反应。
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calcium channel blocker
- Deborah A. Goldspink, .et al. Mechanistic insights into the detection of free fatty and bile acids by ileal glucagon-like peptide-1 secreting cells, Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
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Calcium channel blocker
Clevidipine是一种二氢吡啶类钙通道阻滞剂,用于在口服治疗不可行或不理想时降低血压。
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T-type Ca2+ channel blocker
ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
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L-type calcium channel blocker
Amlodipine besylate是一种L型钙通道阻滞剂,具有降压作用。它抑制去极化大鼠主动脉中Ca2 +诱导的收缩(IC50 = 1.9 nM)。
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T-type Ca2+ channel blocker
ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
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Ca2+-dependent blocker
TV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
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K+ channel and CFTR Cl- channel blocker
Glyburide (Glibenclamide) 是一种抗糖尿病化合物,是一类磺脲类药物。
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