GPCR / G Protein

产品 1 到 50 共 86个

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  1. Flopropione

    Catalog No. A16550
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    5-HT1A receptor antagonist/COMT inhibitor
    Flopropione是5-HT1A受体拮抗剂,也是儿茶酚-邻甲基转移酶(COMT)抑制剂。 了解更多
  2. MHP 133

    Catalog No. A20058
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    AChE /M1/M2/5HT4/I2 inhibitor
    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors. 了解更多
  3. Vortioxetine

    Catalog No. A21266
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    5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor
    Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. 了解更多
  4. Vilazodone D8

    Catalog No. A21876
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    SSR inhibitor / 5-HT1A receptor partial agonist
    Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. 了解更多
  5. Eplivanserin mixture

    Catalog No. A21987
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    serotonin reuptake inhibitor/5-HT2A receptor antagonist
    Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. 了解更多
  6. Vilazodone

    Catalog No. A11116
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    Serotonin reuptake 抑制剂
    Vilazodone充当5-羟色胺再摄取抑制剂(IC50 = 0.5 nM)和5-HT1A受体部分激动剂(IC50 = 0.2 nM; IA =?60-70%)。 了解更多
  7. Sibutramine hydrochloride

    Catalog No. A12397
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    SNR 抑制剂
    Sibutramine hydrochloride是5-HT和去甲肾上腺素再摄取抑制剂(SNRI)。 了解更多
  8. Levomilnacipran HCl

    Catalog No. A14391
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    serotonin/NE reuptake 抑制剂
    Levomilnacipran HCl是一种选择性的5-羟色胺和去甲肾上腺素再摄取抑制剂。 了解更多
  9. Edivoxetine HCl

    Catalog No. A13865
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    norepinephrine reuptake 抑制剂
    Edivoxetine HCl是一种选择性去甲肾上腺素再摄取抑制剂。 了解更多
  10. Norfluoxetine

    Catalog No. A13458
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    serotonin uptake 抑制剂
    Norfluoxetine是抗抑郁药氟西汀的活性代谢物,抑制5-羟色胺的摄取,pKi值为7.35.1氟西汀的S-对映体的5-羟色胺再摄取阻断能力是R-对映体的20倍(pKis分别为7.86和6.51)。 了解更多
  11. Atomoxetine HCl

    Catalog No. A13424
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    norepinephrine (NE) transporter 抑制剂
    Atomoxetine HCl是SLC6A2的一种竞争性特异性抑制剂,同时在大鼠下丘脑突触体中显示出微弱的ST和DAT抑制作用。 了解更多
  12. Asenapine HCl

    Catalog No. A15002
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    adrenergic receptor/5-HT receptor 抑制剂
    Asenapine hydrochloride抑制肾上腺素能受体(α1,α2A,α2B,α2C)的Ki为0.25-1.2 nM,还抑制5-HT受体(1A,1B,2A,2B,2C,5A,6、7),Ki为0.03- 4.0 nM。 了解更多
  13. Desvenlafaxine succinate hydrate

    Catalog No. A15491
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    serotonin (5-HT)/norepinephrine (NE) reuptake 抑制剂
    Desvenlafaxine succinate hydrate是一种新型5-羟色胺(5-HT)转运蛋白 和去甲肾上腺素(NE)转运蛋白重吸收抑制剂,Ki值分别为40.2 nM和558.4 nM 了解更多
  14. YL-0919

    Catalog No. A16337
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    5-HT1A receptor 激动剂/serotonin reuptake 抑制剂
    YL0919,具有5-HT1A受体激动剂和选择性5-羟色胺再摄取抑制剂双重活性的新型抗抑郁候选药物,YL-0919抑制5-HT被大鼠大脑皮层突触小体和人重组细胞摄取的IC50值为1.78±0.34 nM和1.93±0.18 nM。 了解更多
  15. Eucalyptol

    Catalog No. A15662
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    5-HT3 receptor 抑制剂
    Eucalyptol是一种在桉树和其他植物中发现的双环单萜。它是5-HT3受体,钾通道,TNF-α的抑制剂。和IL-1β。 了解更多
  16. Nefazodone hydrochloride

    Catalog No. A17622
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    5-HT2 receptors inhibitor
    Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test. 了解更多
  17. Asenapine

    Catalog No. A18010
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    adrenergic receptor inhibitor
    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. 了解更多
  18. Apalutamide (ARN-509)

    Catalog No. A11923
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    Androgen Receptor 抑制剂
    Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂,IC50 为 16 nM。ARN-509与靶组织中的AR结合,从而阻止了雄激素诱导的受体激活,并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。 了解更多
  19. Phenoxybenzamine hydrochloride

    Catalog No. A10719
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    α-adrenergic (AR) 拮抗剂/CaM 抑制剂
    Phenoxybenzamine hydrochloride是一种细胞可渗透的,非特异性的,不可逆的α-肾上腺素(AR)拮抗剂,也可作为CaM抑制剂。 了解更多
  20. Maprotiline hydrochloride

    Catalog No. A10555
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    noradrenalin re-uptake 抑制剂
    Maprotiline hydrochloride是选择性去甲肾上腺素再摄取抑制剂。 了解更多
  21. Anisodamine

    Catalog No. A18215
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    alpha-1 adrenergic receptors / mAChRs inhibitor
    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant. 了解更多
  22. Orphenadrine citrate

    Catalog No. A11712
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    NMDA receptor 拮抗剂
    Orphenadrine柠檬酸盐是NMDA受体拮抗剂,Ki为6.0μM,还是HERG钾离子通道阻断剂。 了解更多
  23. Rupatadine Fumarate

    Catalog No. A12356
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    PAFR 抑制剂/H1 receptor 抑制剂
    Rupatadine Fumarate是PAFR和组胺(H1)受体的抑制剂,Ki分别为550和102 nM。 了解更多
  24. Rupatadine

    Catalog No. A11222
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    PAFR 抑制剂/H1 receptor 抑制剂
    Rupatadine是PAFR和组胺(H1)受体的抑制剂,Ki分别为550和102 nM。 了解更多
  25. Fexofenadine HCl

    Catalog No. A11859
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    COX 抑制剂/histamine H1 receptor 激动剂
    Fexofenadine Hydrochloride是一种抗组胺药,可抑制Cox-1,Cox-2,并且是组胺H1受体激动剂,IC50为246 nM。 了解更多
  26. Antazoline HCl

    Catalog No. A16411
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    Histamine H1 receptor 抑制剂
    Antazoline HCl是第一代抗组胺药,可与组胺H1受体结合并阻断内源性组胺的作用。 了解更多
  27. Azatadine dimaleate

    Catalog No. A16418
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    Histamine/cholinergic 抑制剂
    Azatadine是一种组胺和胆碱能抑制剂,IC50分别为6.5 nM和10 nM。 了解更多
  28. Nepicastat (free base) (SYN-117)

    Catalog No. A10637
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    dopamine beta-hydroxylase 抑制剂
    Nepicastat (free base) (SYN-117)是多巴胺β-羟化酶的抑制剂,该酶催化多巴胺向去甲肾上腺素的转化。 了解更多
  29. Phenylpiracetam

    Catalog No. A15211
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    Dopamine reuptake 抑制剂
    Phenylpiracetam是促智药物吡乙酰胺的苯基化衍生物。它被用作促智药物,效力比吡乙酰胺高30-60倍。 了解更多
  30. Loxapine Succinate

    Catalog No. A17347
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    D2DR and D4DR inhibitor
    Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia. 了解更多
  31. Promazine hydrochloride

    Catalog No. A17638
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    D2DR inhibitor
    Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity. 了解更多
  32. Zamicastat

    Catalog No. A13672
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    dopamine β-hydroxylase (DBH) inhibitor
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. 了解更多
  33. Pentiapine

    Catalog No. A12512
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    dopamine release inhibitor
    Pentiapine is a novel dopamine release inhibitor. 了解更多
  34. Loxapine

    Catalog No. A18073
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    D2DR/D4DR inhibitor
    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. 了解更多
  35. Vanoxerine

    Catalog No. A21922
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    dopamine reuptake inhibitor
    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). 了解更多
  36. GBR 12935

    Catalog No. A21951
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    dopamine reuptake inhibitor
    GBR 12935 is a potent, and selective dopamine reuptake inhibitor. 了解更多
  37. Radafaxine hydrochloride

    Catalog No. A20951
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    dopamine transporter/norepinephrine transportertransporters inhibitor
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator. 了解更多
  38. Vanoxerine 2HCl (GBR-12909)

    Catalog No. A10725
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    dopamine re-uptake 抑制剂
    Vanoxerine 2HCl (GBR-12909)是哌嗪衍生物,是一种有效的、选择性的多巴胺摄取(dopamine uptake)抑制剂。 了解更多
  39. Lurasidone (SM13496)

    Catalog No. A11214
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    Dopamine D2 抑制剂
    Lurasidone (SM-13496)是dopamine D2和5-HT7的拮抗剂,IC50 值分别为 1.68 和 0.495 nM。Lurasidone (SM-13496) 也是 5-HT1A 受体的部分激动剂。 了解更多
  40. GBR-12935 2HCl

    Catalog No. A11937
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    DAT and SLC6A2 抑制剂
    GBR-12935 dihydrochloride是一种有效的选择性多巴胺再摄取抑制剂。 了解更多
  41. Haloperidol (Haldol)

    Catalog No. A10446
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    CYP2D6 抑制剂
    Haloperidol (Haldol)是一种抗精神病药和丁二酮。 了解更多
  42. GBR 12783 dihydrochloride

    Catalog No. A13128
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    dopamine uptake 抑制剂
    GBR 12783 dihydrochloride是一种非常有效的选择性多巴胺摄取抑制剂(抑制大鼠纹状体突触体中[3H]-多巴胺摄取的IC50为1.8 nM)。 了解更多
  43. Bupropion

    Catalog No. A15850
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    NDR 抑制剂
    Bupropion是主要用作抗抑郁药和戒烟辅助药的药物。 了解更多
  44. (-)-Huperzine A

    Catalog No. A10006
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    GluR 抑制剂
    (-)-Huperzine A是一种天然存在的倍半萜生物碱化合物,存在于石楠石杉中。 了解更多
  45. LDE225 Diphosphate

    Catalog No. A12774
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    Smoothened 抑制剂
    LDE225 Diphosphate 是一种具有潜在抗肿瘤活性的口服生物利用小分子平滑(Smo)拮抗剂。抑制Hedgehog (Hh)信号通路,无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。 了解更多
  46. PF-5274857

    Catalog No. A12775
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    Smoothened 抑制剂
    PF-5274857是一种新型Smo拮抗剂,它以4.6±1.1 nmol/L的K(i)特异性结合Smo,并以2.7±1.4 nmol/L的IC(50)完全阻断下游基因Gli1的转录活性。在细胞中。 了解更多
  47. BMS-833923 (XL-139)

    Catalog No. A13204
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    Smoothened 抑制剂
    BMS-833923 (XL-139)是一种生物可利用的小分子SMO(平滑)抑制剂,具有潜在的抗肿瘤活性。 了解更多
  48. Glasdegib (PF-04449913)

    Catalog No. A13881
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    Smoothened 抑制剂
    PF-04449913是有效且口服可生物利用的平滑化抑制剂。 了解更多
  49. Jervine

    Catalog No. A16221
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    SMO 抑制剂
    Jervine是天然存在的甾体生物碱,可通过阻断声波刺猬(Shh)信号传导而引起Cyclopia。抑制Smo。 了解更多
  50. Saridegib

    Catalog No. A12966
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    Smo inhibitor
    Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway. 了解更多

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