T71537
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Tofenacin hydrochloride is an antidepressant drug with a tricyclic-like structure. It acts as a serotonin-norepinephrine reuptake inhibitor, and based on its close relation to orphenadrine, may also possess anticholinergic and antihistamine properties. Tofenacin is also the major active metabolite of orphenadrine and likely plays a role in its beneficial effects against depressive symptoms seen in Parkinson's disease patients. |
T60430
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Protriptyline 是有效的抗抑郁剂,抑制AChE 活性(IC50 =.06 mM),并可抑制 Aβ 自组装。Protriptyline 具有用于抑郁症和阿尔茨海默病的研究潜力。 |
T0204
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5-HT Receptor
AChE
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Protriptyline hydrochloride (Protriptyline HCl) 是一种含有一个仲胺的三环结构抗抑郁试剂,可以用于抑郁和 ADHD 的相关研究。它使动物精力充沛起激励作用,并且有时用于嗜睡症的相关研究。 |
T60471
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Lanicemine (AZD6765) dihydrochloride 是NMDA 通道的低捕获拮抗剂,Ki 值为 0.56-2.1 μM,在CHO 和爪蟾卵母细胞的IC50分别为 4-7 μM 和 6.4 μM。Lanicemine (AZD6765) dihydrochloride 具有持续的抗抑郁功效。 |
T38228
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High affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable.
Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216 |Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 180 215 PMID:15696320 |Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID:12538845 |Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID:12093593 |
T75944
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Spadin TFA 是一种从血液中释放的前肽衍生的天然肽,是一种有效的 TREK-1 通道阻滞剂,其 IC50值为 10 nM。Spadin TFA 增强小鼠中缝背核 5-HT 神经传递,诱导海马 CREB 激活和神经发生。Spadin TFA 可用于抗抑郁研究。 |
T60576
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Cyproheptadine 是一种有效的口服活性5-HT2A 受体拮抗剂。Cyproheptadine 具有抗抑郁和抗血清素作用。Cyproheptadine 还具有抗血小板和血栓保护活性,可用于研究血栓栓塞性疾病。 |
T83676
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Tianeptine metabolite MC5是一种来自非典型抗抑郁化合物tianeptine的活性代谢物,通过β-氧化形成。此代谢物在使用表达人类μ-阿片受体(MOR)而非人类δ-阿片受体(DOR;EC50s = 0.454和 >100 µM, 分别)的HEK293T细胞进行的生物发光共振能量转移(BRET)试验中,特异性诱导G蛋白激活。在野生型小鼠上,30 mg/kg剂量的Tianeptine metabolite MC5可减少强迫游泳测试中的静止时间,但在MOR敲除小鼠中则不会,表明其具有MOR依赖的抗抑郁样活性。 |
T2579
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Norepinephrine
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Reboxetine (Norebox) 是一种抗抑郁药,用于治疗临床抑郁症、恐慌症和 ADD/ADHD。它有两个手性中心,但它仅作为两种对映体存在,(R, R)-(-)- 和 (S, S)-(+)-Reboxetine。 |
T75895
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UFP-101 TFA 是一种强效、选择性和竞争性的 NOP 受体拮抗剂,pKi 为 10.24。UFP-101 TFA 对 δ、μ 和 κ 类阿片受体的选择性大于 3000 倍。UFP-101 TFA 具有抗抑郁药样作用。 |