T72220
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DSP-1053 是一种苄基哌啶衍生物,一种有效的血清素转运蛋白 (SERT) 抑制剂,Ki 值为 1.02 nM。DSP-1053 显示5-HT1A 受体部分激动活性,Ki 值为 5.05 nM。DSP-1053 具有抗抑郁活性。 |
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。 |
T69019
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Mecamylamine 是一种具有口服活性,非选择性,非竞争性的nAChR 拮抗剂。Mecamylamine 也是一种神经节阻滞剂,可穿过血脑屏障。Mecamylamine 可用于神经疾病,高血压,抗抑郁的研究。 |
T60235
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(Rac)-Lanicemine ((Rac)-AZD6765) 是 Lanicemine 的外消旋体。Lanicemine (AZD6765) 是一种低捕获的NMDA 受体拮抗剂,Ki 为 0.56-2.1 μM;在CHO 和非洲爪蟾卵母细胞中,IC50分别为 4-7 μM 和 6.4 μM。Lanicemine 具有抗抑郁作用。 |
T61617
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Hcyb1 is a potent and specific inhibitor of phosphodiesterase 2 (PDE2). It exhibits a high degree of selectivity for inhibiting PDE2A with an IC50 value of 0.57 μM. In addition, Hcyb1 displays over 250-fold selectivity against other recombinant members of the PDE family. Moreover, its pharmacological actions include neuroprotective and antidepressant-like effects, which are believed to be mediated through the cAMP/cGMP-CREB-BDNF signaling pathway [1]. |
T71302
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Norfluoxetine-d5 is intended for use as an internal standard for the quantification of norfluoxetine by GC- or LC-MS. Norfluoxetine is an active metabolite of the antidepressant fluoxetine. It is formed from fluoxetine by the cytochrome P450 (CYP) isoforms CYP2C9, CYP2C19, and CYP3A. Norfluoxetine inhibits serotonin (5-HT) uptake in rat brain synaptosomal membrane preparations (Ki = 44.7 nM) and isolated human platelets (IC50 = ~15 nM). It has been found in the tissues of fish exposed to wastewater effluent. |
T70183
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Eptapirone, also known as F11440, is a potent 5HT(1A) receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). |
TMIH-0605
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Vortioxetine-d8 2HBr 是 Vortioxetine 2HBr 的氘代化合物。Vortioxetine 2HBr 的 CAS 号为 508233-74-7。Vortioxetine 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和 5-羟色胺转运体抑制剂,Ki值分别为 15、33、3.7、19 和 1.6 nM。它作为抗抑郁药,用于治疗重度抑郁症。 |
T72209
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(R,R)-Reboxetine mesylate 是一种抗抑郁药,具有良好的生物利用度。(R,R)-Reboxetine 为 Reboxetine 的对映体之一,属于选择性去甲肾上腺素再摄取抑制剂。Reboxetine 本身包含 (R,R) 与 (S,S) 两种对映体,且对 α-肾上腺素能和毒蕈碱受体的亲和力较低,表现出较低的动物毒性。 |
T78869
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Potassium Channel
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TWIK-1/TREK-1-IN-2(Compound 2g)为特异性TWIK-1/TREK-1抑制剂,其针对TREK-1同二聚体的IC50值为10.13 μM,以及针对TWIK-1/TREK-1异二聚体的IC50为15.5 μM,表现为潜在的抗抑郁化合物。 |