Membrane Transporters/Ion Channels
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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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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
- 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
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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Lacidipine是一种钙通道阻滞剂。
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Benidipine hydrochloride是一种长效的T型钙通道阻滞剂,对高血压糖尿病患者的血压和肾功能有影响。
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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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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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Diethylstilbestrol是一种合成的非甾体雌激素,于1938年首次合成。它也被分类为内分泌干扰物。
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Diltiazem HCl是一种非二氢吡啶(非DHP)药物,称为钙通道阻滞剂,用于治疗高血压,心绞痛和某些类型的心律不齐。
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Manidipine (Manyper)是二氢吡啶化合物和钙通道蛋白抑制剂和拮抗剂。
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Pinaverium Bromide是一种痉挛剂,抗胆碱能作用的发生率低。吡那溴铵也是解痉药。
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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 抑制剂
Nimodipine是一种L型Ca2+通道阻滞剂。
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Selective calcium chelator
BAPTA tetrapotassium是一种选择性钙螯合剂,对Ca2+的亲和力大于Mg2+。
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Selective calcium chelator
BAPTA/AM是一种细胞内钙螯合剂,可通过脂氧合酶介导的自由基在小鼠皮层培养物中诱导延迟性坏死。
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- Liying Wu, .et al. Capsaicin inhibits the stemness of anaplastic thyroid carcinoma cells by triggering autophagy-lysosome mediated OCT4A degradation, Phytother Res, 2022, Feb;36(2):938-950 PMID: 35076979
- Shichen Xu, .et al. Capsaicin induces mitochondrial dysfunction and apoptosis in anaplastic thyroid carcinoma cells via TRPV1-mediated mitochondrial calcium overload, Cell Signal, 2020, Aug 6;75:109733 PMID: 32771398
- Miho Akimoto, .et al. Antidiabetic adiponectin receptor agonist AdipoRon suppresses tumour growth of pancreatic cancer by inducing RIPK1/ERK-dependent necroptosis, Cell Death Dis, 2018, Aug; 9(8): 804 PMID: 30038429
- Zhang L, .et al. Curcumin induces endoplasmic reticulum stress-associated apoptosis in human papillary thyroid carcinoma BCPAP cells via disruption of intracellular calcium homeostasis, Medicine (Baltimore), 2018, Jun;97(24):e11095 PMID: 29901626
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Ca2+ release 抑制剂
Dantrolene是一种肌肉松弛剂,其作用可能是通过消除对ryanodine受体的作用来消除肌肉细胞中的兴奋-收缩偶联。
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Atagabalin与加巴喷丁相关,加巴喷丁同样与α结合。2β钙通道(1和2)。
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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
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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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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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 Activator
Bay K 8644是一种有效的L型Ca2+通道选择性激活剂,IC50为17.3 nM。
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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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Dantrolene sodium是一种骨骼肌松弛剂,其通过干扰肌肉纤维中的激发-收缩偶联起作用。
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CRAC channel 抑制剂
YM-58483是CRAC通道和随后的Ca2+信号的第一个选择性抑制剂。
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Chlorocresol是ryanodine受体的活化剂。
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Cinepazide maleate是Cinepazide的马来酸盐形式,其为血管扩张剂。
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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 antagonist
Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
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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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Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
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L-type calcium antagonist
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
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Calcium channel proteins inhibitor
Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
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Sodium channel blocker
Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.
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voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
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Sodium Channel Nav1.7 inhibitor
Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
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Nav1.7 sodium channel inhibitor
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
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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