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抑制剂&激动剂
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  • 抑制剂&激动剂
    18
    TargetMol | Inhibitors_Agonists
  • 多肽产品
    1
    TargetMol | Peptide_Products
  • OS-3-106
    T89591580000-17-4
    OS-3-106 是一种新型芳酰胺苯基哌嗪,在腺苷酸环化酶抑制试验中作为 D3R 的部分激动剂。
    • ¥ 117
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • MFZ 10-7
    T229761224431-15-5
    MFZ 10-7 是 mGluR5 的负变构调节剂。
    • ¥ 273
    In stock
    规格
    数量
  • LY2940094
    LY-2940094
    T157991307245-86-8
    LY2940094 (LY-2940094) 是一种口服有效的选择性 NOP 受体拮抗剂,可降低动物模型的自身给药酒精依赖,对 NOP 受体具有高亲和力,Ki 为 0.105 nM,和拮抗活力,Kb 为 0.166 nM。
    • ¥ 688
    In stock
    规格
    数量
  • AT-121
    T376102099681-31-7In house
    AT-121 是一种双重μ-阿片和神经肽受体部分激动剂(Kis 分别为 16.49 和 3.67 nM)。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合(EC50s 分别为 19.6 和 34.7 nM)。AT-121(0.003-0.03 mg kg)能以剂量依赖的方式降低辣椒素诱导的热异感,但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中,AT-121 每次注射剂量为 0.3 至 10 μg kg,它缺乏强化作用(一种潜在的滥用标志),不能减少食物颗粒的强化作用。AT-121(0.01 或 0.03 毫克 千克)不会诱发恒河猴的超痛觉,超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药,具有抗伤害和止痛作用。
    • ¥ 2350
    In stock
    规格
    数量
    TargetMol | Inhibitor Hot
  • COR659
    T36520544450-68-2
    COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。
    • ¥ 343
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • 2-fluoro Deschloroketamine hydrochloride
    2-FDCK
    T201352111982-49-1
    2-fluoro Deschloroketamine属于芳基环己胺类化合物,在动物实验中已显示可诱导大鼠进行自我给药行为。
    • 待询
    3-6月
    规格
    数量
  • CMPPE
    T204434841253-81-4
    CMPPE 是一类GABAB受体的正变构调节剂 (PAM),能够抑制大鼠的酒精自我给药及复饮行为。
    • 待询
    10-14周
    规格
    数量
  • JNJ-55511118
    JNJ55511118, JNJ 55511118
    T255582036081-86-2
    JNJ-55511118 是一种具有高效性和选择性的 TARP γ8 负变构调节剂,具有抗惊厥和神经保护活性,通过降低其单通道电导来抑制含有 γ8 的 AMPAR 的峰值电流,可用于研究慢性操作性酒精自我给药。
    • 待估
    35日内发货
    规格
    数量
  • BHF-177
    T26791917896-43-6
    BHF-177 is a positive allosteric modulator of the GABAB receptor. BHF-177 reduces self-administration of nicotine in animal studies.
    • ¥ 10600
    6-8周
    规格
    数量
  • Yhhu 3792
    T35546
    Notch signaling pathway activator; enhances the self-renewal capability of neural stem cells (NSCs) via Notch signaling pathway activation in vitro and in vivo. Promotes the expression of Notch target genes, Hes3 and Hes5. Expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) after chronic administration in mice. Increases the spatial and episodic memory in mice.
    • ¥ 4598
    待询
    规格
    数量
  • Pal-KTTKS (acetate)
    T36929
    Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).
    • 待估
    35日内发货
    规格
    数量
  • CC4
    CC4
    T37202492-02-4
    High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID:22957729 |Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID:16273122 |Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur.J.Pharmacol. 471 85 PMID:12818695
    • 待估
    35日内发货
    规格
    数量
  • Ro60-0175
    Ro60-0175
    T39161169675-08-5
    Ro60-0175 是 5- 羟色胺 2B (5-HT2B) 和 5- 羟色胺 2C (5-HT2C) 血清素受体亚型的选择性激动剂,常用富马酸盐形式。 它具有 5- 羟色胺 2B 受体激动剂和 5- 羟色胺 2C 受体激动剂的作用。
    • ¥ 818
    In stock
    规格
    数量
  • AT-1001
    T709871314801-63-2
    AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.
    • ¥ 10600
    6-8周
    规格
    数量
  • AZD-8418
    T712621198309-73-7
    AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by chronic AZD8529 administration persisted throughout the 14 days of treatment. Chronic treatment with either PAMs inhibited food self-administration. AZD8418 (acute) and AZD8529 (acute and subchronic) blocked cue-induced reinstatement of nicotine- and food-seeking behavior.
    • ¥ 10600
    6-8周
    规格
    数量
  • AEF0117
    T799091610878-71-1
    AEF0117为一种针对大麻素受体1 (CB1-SSi) 的信号传导特异性抑制剂,抑制大麻素自我给药和与四氢大麻酚相关的行为障碍,可用于研究大麻戒断。
    • ¥ 198
    In stock
    规格
    数量
  • dopamine d3 receptor agonist 13a
    T837762899250-94-1
    Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合,相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM,分别)具有更高的亲和力,并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM,分别)结合;然而,它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM,在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上,当剂量为3 mg kg时,Dopamine D3 受体激动剂13a能减少可卡因自我给药。
    • 待估
    35日内发货
    规格
    数量
  • KK-92A
    T89401
    KK-92A为穿透血脑屏障的GABAB阳性异构调节剂,能够抑制大鼠自主摄取酒精以及对酒精寻求的提示诱导复发行为.
    • 待询
    规格
    数量
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