Membrane Transporters/Ion Channels
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CaCCs 抑制剂
CaCCinh-A01抑制人支气管和肠道细胞中的CaCC电流。还抑制TMEM16A通道(表达TMEM16A的FRT细胞中IC50 = 2.1 uM)。
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TMEM16A 抑制剂
T16Ainh-A01是一种选择性TMEM16A钙激活的氯离子通道抑制剂,可强烈抑制唾液腺细胞中的氯离子电流。
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CaCC activator
Eact激活钙激活的氯离子通道(CaCC)TMEM16A CaCC。
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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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potassium-competitive acid Blocker
TAK-438 (vonoprazan)是一种新型的钾竞争酸阻滞剂。
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KCa3.1 channel activator
NS 309是小和中电导Ca2+激活的K+通道(KCa2和KCa3.1通道)的正调制器。
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Kir6.2/SUR 抑制剂
Glimepiride是一种强效Kir6.2/SUR抑制剂,SUR1、SUR2A和SURB的IC50分别为3.0 nM、5.4 nM和7.3 nM,用于治疗2型糖尿病化合物。
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Retigabine是一种新型的抗痉挛剂,在大范围的惊厥模型具有活性。其发挥活性的机制主要是开放神经元的KCNQ2-5电压门控钾离子通道。
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- Sotatsu Tonomura, .et al. Function of KCNQ2 channels at nodes of Ranvier of lumbar spinal ventral nerves of rats, Mol Brain, 2022, Jul 20;15(1):64 PMID: 35858950
- Vigil FA, .et al. Prevention of brain damage after traumatic brain injury by pharmacological enhancement of KCNQ (Kv7, ??M-type??) K+ currents in neurons, J Cereb Blood Flow Metab, 2019, Jul 4:271678X19857818 PMID: 31272312
- Joseph Lombardo, .et al. Nonreciprocal mechanisms in up- and downregulation of spinal motoneuron excitability by modulators of KCNQ/Kv7 channels, J Neurophysiol, 2016, Nov 1; 116(5): 2114-2124 PMID: 27512022
- Sonya M. Bierbower, .et al. Augmentation of M-Type (KCNQ) Potassium Channels as a Novel Strategy to Reduce Stroke-Induced Brain Injury, J Neurosci, 2015, Feb 4; 35(5): 2101-2111 PMID: 25653366
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Hydralazine hydrochloride是肼屈嗪的盐酸盐(安普索林),是一种直接作用的平滑肌松弛剂,IC50为1.9 mM。
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Minoxidil (U-10858)是一种选择性的ATP依赖性K+(Kir6)通道激活剂。
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Nateglinide(Starlix)是一种胰岛素促分泌剂,可通过刺激胰腺分泌胰岛素来降低血糖水平。
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KATP channel 拮抗剂
Mitiglinide calcium是一种降血糖药物,通过关闭胰腺β细胞中的ATP敏感K+通道来刺激胰岛素分泌。
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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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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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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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Kir6 (KATP) channel opener
Nicorandil (SG-75) 钾离子通道活化剂。
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Potassium Channel 抑制剂
Repaglinide是一种有效的短效胰岛素促分泌剂,可通过关闭胰岛β细胞质膜中的ATP敏感性钾(KATP)通道发挥作用。
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KCa2.1 channels activator
GW 542573X是小电导Ca2+激活的K+通道(KCa2)的激活剂。
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20-HETE是在血管平滑肌(VSM)细胞中产生的有效血管收缩剂。
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KCNQ channel opener
Retigabine dihydrochloride是具有抗惊厥活性的Kv7.2-7.5(KCNQ2-5)神经元钾通道开放剂。
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hERG1 potassium channel activator
KB130015是hERG1钾离子通道的新型激活剂,可在高压下阻断天然和重组hERG1通道,但在低压下激活它们。
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KV7.2/7.3 activator
ICA-110381是KV7.2/7.3激活剂,EC50为0.38 uM。
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hERG channel activator
NS-1643是一种人类以太相关基因(hERG)KV11.1通道激活剂(EC50 = 10.5 uM)。
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Potassium channel activator
NS1619是Bkca开启剂或大电导Ca2+激活的钾(BKCa,KCa1.1)通道激活剂。
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Doxapram能抑制TASK-1,TASK-3,TASK-1/TASK-3异二聚体通道功能,EC50分别为410 nM,37μM,9μM。Doxapram是一种呼吸刺激剂。静脉注射多沙普兰可刺激潮气量和呼吸频率的增加。
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K+ Channel 抑制剂
K+ Channel inhibitor,Kv1.5(IKur)的二氢吡唑并嘧啶抑制剂的合成基础。
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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 channel activator
SKA-31是KCa2和KCa3.1钙激活钾通道的激活剂。
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Potassium channel blocker
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk.
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Kv3 potassium channel modulator
AUT1 is a Kv3 potassium channel modulator with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
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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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K+ (KATP) channel activator
Y-26763 is a K+ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K+ (KATP) channel activator.
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IKs blocker
JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
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HERG activator
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
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ROMK inhibitor
MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
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hERG potassium channel inhibitor
Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
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potassium channel inhibitor
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
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KCNQ1 potassium channel activator
ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
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Riluzole (Rilutek)阻断与受损神经元有关的TTX敏感性钠通道,从而减少钙离子的流入并间接防止谷氨酸受体的刺激。
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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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Lacosamide是一种用于辅助治疗部分发作性癫痫发作和糖尿病神经性疼痛的药物。
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- Yi-Shuan Peng, .et al. Inhibition of neuronal Na+ currents by lacosamide: Differential binding affinity and kinetics to different inactivated states, Neuropharmacology, 2020, Aug 24;179:108266 PMID: 32853658
- Namer B, .et al. Pain relief in a neuropathy patient by lacosamide: Proof of principle of clinical translation from patient-specific iPS cell-derived nociceptors, EBioMedicine, 2018, Nov 28. pii: S2352-3964(18)30546-2 PMID: 30503201
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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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Bupivacaine HCl与化学相关的局部麻醉药相比,Bupivacaine HCl是一种更有效的cAMP抑制剂,较不易产生心血管毒性。
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SGLT2 抑制剂
PF-04971729是钠依赖性葡萄糖共转运蛋白2的有效和选择性抑制剂。
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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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Voltage-gated sodium channels 拮抗剂
Proparacaine HCl是一种电压门控钠通道拮抗剂,ED50为3.4 mM。
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Amiloride hydrochloride dihydrate是一种强效上皮钠通道阻滞剂和选择性低阈值(t型)钙通道蛋白抑制剂(kd=30μm)。
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Ibutilide fumarate是一种III类抗心律失常药,用于房颤的急性心脏转换和近期发作的心房扑动转为窦性心律。它通过诱导缓慢的内向钠电流发挥抗心律失常作用,延长心肌细胞的动作电位和不应期(生理学)。
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Carbamazepine是一种抗惊厥和稳定情绪的药物,主要用于治疗癫痫和双相情感障碍以及三叉神经痛。
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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Lidocaine (Alphacaine)是一种麻醉剂和Ib类抗心律失常药。在失活状态下阻断电压门控钠通道。
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