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抑制剂&激动剂
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  • 抑制剂&激动剂
    14
    TargetMol | Inhibitors_Agonists
  • 多肽产品
    4
    TargetMol | Peptide_Products
  • 天然产物
    3
    TargetMol | Natural_Products
  • Glycyl-L-Histidyl-L-Lysine
    T450849557-75-7
    Glycyl-L-Histidyl-L-Lysine 是一种肝细胞生长因子和一种合成的肝营养剂,可刺激肝红细胞生成因子的产生。
    • ¥ 99
    In stock
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  • SB-224289 hydrochloride
    SB-224289A
    T12841180084-26-8In house
    SB-224289 hydrochloride (SB-224289A) 是一种选择性的 5-HT1B receptor 拮抗剂,具有抗焦虑作用。
    • ¥ 209
    In stock
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  • orcinol
    苔黑素、苔黑酚、地衣酚, 5-Methylresorcinol, 5-Methylresorcin, 5-Methyl-1,3-benzenediol, 3,5-ToluenediolOrcin, 3,5-Dihydroxytoluene
    T3748504-15-4
    orcinol (5-Methylresorcin) 可用于生物染料和蛋白质组学研究。
    • ¥ 108
    In stock
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  • Pulegone
    蒲勒酮,胡薄荷酮,长叶薄荷酮, 胡薄荷酮, (+)-Pulegone
    TCS010289-82-7
    Pulegone ((+)-Pulegone) 是 Calamintha nepeta (L.) Savi 的精油的主要化学成分,也是禽类驱虫剂之一。它在禽类物种中驱避作用的分子靶点是伤害感受性 TRP 锚蛋 1。它刺激鸡感觉神经元中的 TRPM8 和 TRPA1 通道,并在高浓度下抑制前者但不抑制后者。
    • ¥ 108
    In stock
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  • 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
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  • Valepotriate
    Valtrate, 戊曲酯 缬草素
    T4S199918296-44-1
    Valepotriate (Valtrate) 是从蜘蛛香分离而来的一种天然产物,是一类新的细胞毒剂和抗肿瘤剂,对 HTC 肝癌细胞是非常有效的细胞毒剂。 它可能对焦虑的精神症状具有潜在的抗焦虑作用。
    • ¥ 552
    In stock
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  • Etifoxine hydrochloride
    盐酸艾替伏辛, HOE 36-801 hydrochloride
    T1369056776-32-0
    Etifoxine hydrochloride (HOE 36-801 hydrochloride) 是GABAA 受体亚基 α1β2γ2 和 α1β3γ2 的阳性变构调节剂,是具有 GABA 能的非苯二氮卓类抗焦虑和抗惊厥药物。
    • ¥ 145
    In stock
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    TargetMol | Inhibitor Sale
  • CVT-10216
    3-[[[3-[4-[(甲基磺酰基)氨基]苯基]-4-氧代-4H-苯并吡喃-7-基]氧基]甲基]苯甲酸
    T150221005334-57-5
    CVT-10216 是可逆的、选择性的醛脱氢酶 2(ALDH-2)抑制剂,IC50为 29 nM。对 ALDH-1的抑制作用较弱,IC50为 1.3 μM。 它可以减少偏爱酒精的大鼠过量饮酒,并表现出抗焦虑作用。
    • ¥ 538
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  • Betamethasone 21-phosphate (sodium salt hydrate)
    T38100
    Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)
    • 待估
    35日内发货
    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
  • Phoenixin-14
    PNX-14
    T804221415039-79-0
    Phoenixin-14 (PNX-14) 是一种具有内源性活性的异构体,能通过激活AHA GnRH系统发挥抗焦虑效果,并抑制缺血 再灌注所诱导的小胶质细胞毒性。
    • 待询
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  • Phoenixin-20
    PNX-20
    T804231415039-77-8
    Phoenixin-20(PNX-20)为脊椎动物内具激素样生物活性肽,能激活下丘脑-垂体-性腺轴,调控哺乳类生殖过程。该肽通过CREB-PGC-1α途径增进神经元线粒体生物发生。
    • 待询
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  • MCL0020
    MCL 0020
    TP1889475498-26-1
    MCL0020 是一种有效的选择性黑素皮质素MC4受体拮抗剂,IC50为 11.63 nM。它剂量依赖性减轻束缚应激诱发的厌食症,在体内表现出抗焦虑样活性。
    • ¥ 1120
    In stock
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  • tandospirone
    坦度螺酮, SM-3997, SM3997
    TQ031587760-53-0
    Tandospirone (SM-3997) 是一种具有选择性和高效性的 5-HT1A 受体部分激动剂,具有抗焦虑和抗抑郁活性,增强缬沙坦对自发性高血压大鼠的抗心肌纤维化作用,可用于研究中枢神经系统疾病。
    • ¥ 198
    In stock
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