Cat. No. | Product Name | Target | Signaling Pathways |
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T15795 |
Luzindole
N-乙酰-2-苄基色胺,N-0774 |
Melatonin Receptor; MT Receptor | GPCR/G Protein; Neuroscience |
Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂,可抑制实验性自身免疫性脑脊髓炎,有抗抑郁样活性。它优先靶向 MT2 (Mel1b),对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。 | |||
T23394 |
SR 57227A
SR57227盐酸盐,SR 57227 hydrochloride |
5-HT Receptor | GPCR/G Protein; Neuroscience |
SR 57227A (SR 57227 hydrochloride) 是一种有效的、具有口服活性和选择性的 5-HT3 受体激动剂,具有穿越血脑屏障的能力和抗抑郁作用。它对大鼠皮质膜和整个 NG 108-15 细胞或其膜上的 5-HT3 受体结合位点的亲和力,IC50在 2.8 至 250 nM 之间。 | |||
T38007 |
Noladin ether
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Noladin ether 是一种选择性的大麻素 CB1 受体激动剂(Ki=21.2 nM)。Noladin ether 可导致体温过低、肠道不动和轻度的缓解疼痛作用。 | |||
T80693 |
β-Endorphin, rat
β-Lipotropin 61-91 |
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β-Endorphin, rat (β-Lipotropin 61-91) 是一种在心血管调节中起作用的神经肽。该化合物能导致大鼠出现显著的持续性肌肉僵硬和静止,这种效应与紧张状态相似。 | |||
T38109 |
Galanin (2-11) amide (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)
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Galanin (2-11) amide is a synthetic peptide fragment of the neuropeptide galanin and an agonist of the galanin-2 (GAL2) receptor (EC50= 9.32 nM in a fluorescence imaging plate reader assay).1It selectively binds to the GAL2receptor (IC50= 1.76 nM for the rat receptor) over the GAL1receptor (IC50= 879 nM for the human receptor) but does also bind to the GAL3receptor (Ki= 271 nM for the rat receptor).1,2Intracerebroventricular administration of galanin (2-11) amide (1 nmol/animal) decreases immobi... | |||
T83676 |
Tianeptine Metabolite MC5 sodium
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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。 | |||
T83733 |
TIP39 (human, bovine) TFA
Tuberoinfundibular Peptide of 39 Residues |
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TIP39作为一种神经肽及甲状旁腺激素受体2型(PTH2R)激动剂,在表达重组人或大鼠PTH2R的COS-7细胞中诱导cAMP积累(EC50分别为0.5和0.8 nM),以及在内源性表达PTH2R的F-11细胞中(EC50 = 1.15 nM)。在CFK2大鼠软骨细胞中,TIP39 (1 nM)诱导细胞周期在G0/G1阶段停滞,并减少软骨分化的主要调控因子Sox9的表达。此外,TIP39 (100 pmol/动物)在小鼠强迫游泳测试中减少了不动时间。 | |||
T36521 |
Alaproclate (hydrochloride)
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Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio... | |||
T37194 |
5α-Androst-16-en-3α-ol
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5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg/kg) decreases immobility time in the forced s... |