“angiotensin converting enzyme ace”的搜索结果
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BACE1 inhibitor
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
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BACE-1 inhibitor
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively.
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AChE inhibitor
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines.
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BACE1 inhibitor
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
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AChE inhibitor
(??)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
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mAChR agonist
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist.
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mAChR M5 negative allosteric modulator
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
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γ-Aminobutyric acid B GABA(B) receptor antagonist
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist.
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α4β2 nAChR partial agonist
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist.
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BACE-1 inhibitor
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
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mAChR modulator
Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
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BACE1 inhibitor
BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively.
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muscarinic acetylcholine receptor (mAChR) antagonist
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
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GABA receptor agonist
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.
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BACE1 inhibitor
Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
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COX-1/COX-2 inhibitor
Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.
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AChE /M1/M2/5HT4/I2 inhibitor
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
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AChE inhibitor
Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM.
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BACE1 inhibitor
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer??s disease.
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P2Y12 platelet inhibitor
Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis.
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alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
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NMDA antagonist
AZD-4282, also known as aminoacetic acid and glycine, is a N-methyl-D-aspartate (NMDA) receptor antagonist potentially for the treatment of neuropathic pain.
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acetylcholinesterase inhibitor
Edrophonium Chloride, also known as Tensilon, is an acetylcholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. Edrophonium Chloride has also been used as an antidote to curare principles.
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COX-2 抑制剂
Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
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AChE & butyrylcholinesterase inhibitor
Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively).
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Acetylcholine iodide是一种神经递质,存在于神经肌肉接头,植物神经节,副交感神经效应接头,交感神经效应接头的子集以及中枢神经系统的许多部位。
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CaMKK 抑制剂
STO-609是钙/钙调蛋白依赖性激酶激酶(CaMKK)亚型CaMKKα和CaMKKβ(Ki分别为80和15 ng/ml)的细胞渗透性抑制剂。
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β-secretase/BACE1 抑制剂
Verubecestat (MK-8931)是一种有效的选择性β-分泌酶抑制剂,是BACE1蛋白抑制剂或Beta-site APP裂解酶1抑制剂。
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γ-secretase 抑制剂
Begacestat (GSI-953)是一种新型的选择性淀粉样前体蛋白γ-分泌酶的噻吩磺酰胺抑制剂。
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BACE1 抑制剂
Timosaponin B-II是知母草(Liliaceae,根茎)的主要活性成分,对脑缺血性损伤具有保护作用。
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BACE1 抑制剂
AMG-8718是一种有效的BACE1抑制剂。
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Oxiracetam是γ-氨基丁酸(GABA)的环状衍生物。
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COX 抑制剂
Acetaminophen (paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂,IC50 值为 25.8 μM。Acetaminophen 是一种有效的肝 N-乙酰转移酶 2 (NAT2) 抑制剂。它是广泛使用的解热和止痛药。
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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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Oxybutynin (Ditropan)是一种抗胆碱能药物,是一种竞争性的muscarinic acetylcholine receptorM1,M2,和M3拮抗剂,用于缓解尿道和膀胱疾病。
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BACE1 抑制剂
AZD3839是人类BACE1的有效选择性抑制剂,Ki为26.1 nM。
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Jaceosidin是一种来源于艾蒿的药理活性黄酮,通过阻断培养的人乳腺上皮细胞中erk-1和-2的磷酸化来抑制佛波酯诱导的cox-2和MMP-9的上调。
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Phenacetin是一种非阿片类镇痛药,无抗炎特性。
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BACE1 抑制剂
LY2811376是第一种可口服的非肽类BACE1抑制剂,可在动物体内产生显着的Aβ降低作用。
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COX 抑制剂
Acemetacin (Emflex)是一种非甾体类抗炎药,是吲哚美辛的乙醇酸酯,是一种环加氧酶抑制剂。
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Gamma-secretase 抑制剂
Semagacestat (LY450139)是一种针对Aβ42,Aβ40和Aβ38的γ-分泌酶阻滞剂,IC50分别为10.9 nM,12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导,IC50为14.1 nM。
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- Yesuvadian R, .et al. Potent γ-secretase inhibitors/modulators interact with amyloid-β fibrils but do not inhibit fibrillation: a high-resolution NMR study., Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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Nefiracetam (Translon)是认知增强剂。它激活L/N型钙通道,胆碱能,单胺能和GABA能系统。
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Gamma-secretase 抑制剂
BMS-708163 (Avagacestat)是口服生物有效的,选择性的γ-分泌酶抑制剂,作用于Aβ40和Aβ42时,IC50分别为0.3 nM和0.27 nM。
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BACE1 抑制剂
LY2886721是一种有效的,选择性的,口服活性的β位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂。LY2886721是一种新型强效药物,用于治疗阿尔茨海默病的研究。
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- Naomi Ito, .et al. miR-15b mediates oxaliplatin-induced chronic neuropathic pain through BACE1 down-regulation, Br J Pharmacol, 2017, Mar; 174(5): 386-395 PMID: 28012171