目录号 | 产品详情 | 靶点 | |
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T60607 | |||
Dasotraline 是一种三重再摄取抑制剂,可阻断多巴胺 (DA),去甲肾上腺素 (NE) 和血清素5-羟色胺 (5-HT) 转运蛋白,IC50值分别为 4, 6 和 11 nM。Dasotraline 代表了一类潜在的新型抗抑郁药。 | |||
T1406L | |||
Amantadine is used both as an antiviral and an anti-parkinsonian drug. Amantadine is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake. The drug has many effects in the brain, including the rel | |||
T76184 | |||
Scyllatoxin (Leiurotoxin I) 为一种从(Leiurus quinquestriatus hebraeus)毒蝎毒液中分离的肽毒素,作为小电导钙激活型钾通道KCa(SK)的阻断剂,有能力增强体内去甲肾上腺素(NE)与肾上腺素(Epi)的释放。 | |||
T60445 | |||
Desipramine 是一种具有抗抑郁活性的三环类化合物。Desipramine 可抑制中枢神经系统的去甲肾上腺素再摄取受体,减少睡眠相关的腮舌肌活性丧失,可用于改善咽塌陷的研究。 | |||
T60509 | |||
Maprotiline 能够抑制细胞的增殖和转移,具有抗癌作用。 Maprotiline 通过靶向 ERK 信号通路和 CRABP1 诱导癌细胞凋亡。 Maprotiline 是一种高度选择性的去甲肾上腺素再摄取阻滞剂,具有有效的抗抑郁作用 [1][2]。 | |||
T83888 | |||
(S)-5-羟基-6-甲氧基Duloxetine是(S)-duloxetine的一个活性代谢物,主要通过对血清素(5-HT)和去甲肾上腺素的再摄取进行抑制。它通过(S)-duloxetine经过一个5-或6-羟基Duloxetine中间体以及一个儿茶酚Duloxetine中间体形成,这些中间体由细胞色素P450 (CYP)同型酶CYP1A2和CYP2D6形成。(S)-5-羟基-6-甲氧基Duloxetine在脂质膜中抑制5-HT转运体(SERT)、去甲肾上腺素转运体(NET)和多巴胺转运体(DAT),其对人类转运体的抑制常数(Kis)分别为266、920和2,814 nM。 | |||
T69104 | |||
SAX-187 hydrochloride is a potent and selective 5-HT6 receptor agonist. SAX-187 hydrochloride possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (SAX-187 hydrochloride: EC50=6.6 nM, Emax=93%). In the rat frontal cortex, acute administration of SAX-187 hydrochloride (3-30 mg/kg, subcutaneous (s.c.)) significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine. | |||
T61008 | |||
(±)-Duloxetine ((Rac)-Duloxetine) hydrochloride 是 Duloxetine hydrochloride 的外消旋物。Duloxetine hydrochloride 可用于研究糖尿病性神经性疼痛、纤维肌痛和重度抑郁症,它是 5-羟色胺去甲肾上腺素再摄取的抑制剂。 | |||
T37167 | |||
Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters). Reduced haloperidol (0.5 mg/kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity. | |||
T60521 | |||
作为三环类抗抑郁药,Doxepin 抑制血清素和去甲肾上腺素的再摄取。Doxepin 具有抗炎作用,可减少抗氧化应激。Doxepin 显示出对特应性皮炎和慢性荨麻疹的治疗效果,并且能改善认知过程和保护中枢神经系统。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-03852 | Dopamine beta-Hydroxylase Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
DBH is a 29 kDa copper-containing oxygenase. It can be detected in noradrenergic nerve terminals of the central and peripheral nervous systems, and is also expressed in chromaffin cells of the adrenal medulla. DBH contains our identical subunits, and its activity requires ascorbate as a cofactor. It functions in in the synthesis of small-molecule neurotransmitters that is membrane-bound, making norepinephrine the only transmitter synthesized inside vesicles. DBH has been shown to be associated with decision making and addictive behaviors such as alcohol and smoking, attention deficit hyperactivity disorder, and also with neurological diseases such as Schizophrenia and Alzheimer's.
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TMPY-02948 | SULT1A3 Protein, Human, Recombinant (His) | Human | E. coli | ||
SULT1A3 belongs to the sulfotransferase 1 family. Sulfotransferase enzymes catalyze the sulfate conjugation of many hormones, neurotransmitters, drugs, and xenobiotic compounds. They are different in their tissue distributions and substrate specificities while their gene structure (number and length of exons) is similar. SULT1A3 gene encodes a phenol sulfotransferase with thermolabile enzyme activity. Four sulfotransferase genes are located on the p arm of chromosome 16; this gene and SULT1A4 arose from a segmental duplication. It is the most centromeric of the four sulfotransferase genes. Exons of this gene overlap with exons of a gene that encodes a protein containing GIY-YIG domains (GIYD1). SULT1A3 is expressed in liver, colon, kidney, lung, brain, spleen, small intestine, placenta and leukocyte. SULT1A3 is a sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic monoamines (neurotransmitters such as dopamine, norepinephrine and serotonin) and phenolic and catechol drugs.
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