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抑制剂&激动剂
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  • 抑制剂&激动剂
    18
    TargetMol | Inhibitors_Agonists
  • 重组蛋白
    1
    TargetMol | Recombinant_Protein
  • 多肽产品
    6
    TargetMol | Peptide_Products
  • 天然产物
    2
    TargetMol | Natural_Products
  • DPN
    Diarylpropionitrile, 2,3-双(4-羟苯基)丙腈
    T76441428-67-7
    DPN (Diarylpropionitrile) 是一种非甾体雌激素受体 ERβ选择性配体,其 EC50值为 0.85 nM。DPN 在许多神经系统疾病具有神经保护作用。
    • ¥ 297
    In stock
    规格
    数量
  • Apigenin
    芹菜素, 金银花, NSC 83244, LY 080400, C.I. Natural Yellow 1, Apigenol, 4',5,7-Trihydroxyflavone
    T2175520-36-5
    Apigenin (LY 080400) 属于黄酮类天然产物,是一种 CYP2C9 抑制剂 (Ki=2 μM),具有竞争性。Apigenin 可以减少焦虑,影响免疫健康,调节激素,被用作镇静剂、温和的镇痛剂和安眠剂。
    • ¥ 333
    In stock
    规格
    数量
  • sb 242084 dihydrochloride
    T371141049747-87-6
    SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg kg i.p., and 2.0 mg kg p.o. SB 242084 (0.1-1 mg kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].
    • ¥ 497
    5日内发货
    规格
    数量
  • TCS 1105
    N-(4-fluorobenzyl)-2-(1H-indol-3-yl)-2-oxoacetamide
    T23444185391-33-7
    TCS 1105是一种GABAA 苯并二氮卓受体(BZR)配体。TCS 1105阻断Sema3A 诱导的轴突生长锥塌陷。TCS 1105能减少小鼠的焦虑样行为,增强攻击性行为和社会支配力。
    • ¥ 173
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • Org-12962
    T16401132834-56-1
    Org-12962 是选择性,具有口服活性的 5-HT2C 受体激动剂,pEC50 值为 7.01。 Org-12962 对 5-HT2A 和 5-HT2B 受体也具有很高的作用,pEC50 分别为 6.38 和 6.28。Org-12962 在焦虑大鼠的模型中显示出缓解作用。
    • ¥ 137
    In stock
    规格
    数量
  • p-MPPI hydrochloride
    T16421220643-77-6
    p-MPPI hydrochloride 是一种选择性的,具有高亲和力的5-HT1A 受体拮抗剂,能穿过血脑屏障,具有抗抑郁和抗焦虑样作用。
    • ¥ 516
    In stock
    规格
    数量
  • Carpipramine maleate
    PZ-1511, PZ1511, PZ 1511, Carpipraminum, Carpipramina, Carbadipimidine
    T202047100482-23-3
    Carpipramine (free base) 在法国和日本用作治疗精神分裂症和焦虑的非典型抗精神病化合物。该化合物除具有神经抑制和抗焦虑效果外,还具有催眠特性。从结构上看,carpipramine 既与三环类化合物如imipramine相似,也与丁酰苯类化合物如haloperidol相关。
    • 待询
    10-14周
    规格
    数量
  • RA-PR058
    T205537
    RA-PR058 是一种 Ramalin 衍生物,具备口服活性及血脑屏障穿透性,具有多靶点调控能力。凭借其优越的药代动力学特性,RA-PR058 通过减少BACE1表达、tau蛋白过度磷酸化和类焦虑行为,展现出作为阿尔茨海默病多靶点调节剂的潜在应用价值。
    • 待询
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  • 6-Hydroxyflavone
    6-羟基黄酮, 6-HF
    T29406665-83-4
    6-Hydroxyflavone (6-HF) 是天然存在的黄酮化合物,具有抗炎作用。它对牛血红蛋白糖基化具有抑制作用。它能激活 AKT、ERK 1 2、JNK 信号通路,有效促进成骨细胞分化。它能抑制 LPS 诱导的 NO 的产生。
    • ¥ 198
    In stock
    规格
    数量
  • 3'-Sialyllactose sodium
    3'-SL sodium
    T35707128596-80-5
    3'-Sialyllactose sodium 是一种益生元,具有抗炎活性,可维持免疫稳态。3'-Sialyllactose sodium 可减少压力源引起的焦虑样行为,可用于研究炎症和关节炎。
    • ¥ 153
    In stock
    规格
    数量
  • Eltoprazine
    T3814598224-03-4
    Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A 1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg kg i.p.) or eltoprazine (1 mg kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.
    • ¥ 10600
    1-2周
    规格
    数量
  • MS21570
    5-(苄基硫代)-N-甲基-1,3,4-噻二唑-2-胺
    T582865373-29-7
    MS21570 作为 GPR171 拮抗剂基于其阻断能力,IC50 为 220 nM,可减少小鼠的焦虑样行为和恐惧条件反射。
    • ¥ 198
    In stock
    规格
    数量
  • Neuropeptide S(Mouse) TFA
    T75950
    Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.
    • 待询
    规格
    数量
  • Neuropeptide S(Rat) TFA
    T75951
    Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.
    • 待询
    规格
    数量
  • α-Helical CRF (9-41) TFA
    α-Helical Corticotropin-Releasing Factor (9-41)
    T83665
    α-Helical CRF (9-41) 是一种合成的皮质酮释放因子(CRF)拮抗剂。它在0.5至5 µM浓度范围内,能抑制CRF诱导的大鼠前叶垂体细胞释放促肾上腺皮质激素(ACTH)。在体内研究中,α-Helical CRF (9-41) (0.02-0.6 µmol/kg) 能够抑制未经麻醉的完整大鼠体内CRF诱导的ACTH释放,并在0.6 µmol/kg剂量下抑制大鼠应激诱导的ACTH释放。此外,α-Helical CRF (9-41) 在尼古丁诱导的条件性焦虑大鼠模型中增加社交互动时间,并减少小鼠的类似暴饮暴食的乙醇消费。
    • 待估
    规格
    数量
  • Neuropeptide S(Mouse)
    Neuropeptide S (Mouse)
    TP1981412938-74-0
    Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.
    • 待估
    35日内发货
    规格
    数量
  • Neuropeptide S(Rat)
    Neuropeptide S (Rat)
    TP1982412938-75-1
    Potent endogenous neuropeptide S receptor (NSPR) agonist (EC50 = 3.2 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.
    • 待估
    35日内发货
    规格
    数量
  • Neuropeptide S (human)
    神经肽S (人类)
    TP1983412938-67-1
    Potent endogenous neuropeptide S receptor agonist (EC50 = 9.4 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.
    • ¥ 2050
    待询
    规格
    数量
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