2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. GSK256471

GSK256471 是一种非肽类速激肽 NK3 受体 (NK3 receptor) 拮抗剂，对人重组 NK3 受体pKi 为 8.9，对豚鼠天然 NK3 受体 pKi 为 8.4。GSK256471 对 NK1 (pKi = 5.2) 和 NK2 (pKi = 7.3) 受体选择性 > 100 倍。GSK256471 可非竞争性抑制 Neurokinin B (NKB) (HY-P0242) 诱导的肌醇磷酸积累，且具有不可逆特性。GSK256471 抑制“湿狗抖擞”行为并抑制多巴胺释放。GSK256471 可用于研究精神分裂症。

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GSK256471

GSK256471 Chemical Structure

CAS No. : 1133706-08-7

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GSK256471 相关抗体

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NK1R NK2R NK3R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia[1][2].

IC50 & Target[2]

NK3R

8.9 (pIC50)

体外研究
(In Vitro)

GSK256471 抑制 NKB 诱导的 U2OS 细胞内钙释放，其 pKi 为 8.9[1]。
GSK256471 (0.01-1 μM) 使 NKB 浓度-反应曲线右移并显著降低最大反应 (Emax)，在 U2OS 细胞中表现出非竞争性拮抗特性[2]。
GSK256471 (0.1-1 μM) 在 U2OS 细胞中完全消除 NKB 引起的神经元放电活动[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GSK256471 相关抗体:
体内研究
(In Vivo)

GSK256471 (1-10 mg/kg，单次静脉注射、口服和腹腔注射) 在大鼠和沙鼠中表现出中等脑部渗透性，但其高亲和力可补偿较低的暴露剂量[1][2]。
GSK256471 (1 ng/kg-100 mg/kg，单次腹腔注射) 在低脑浓度下即可实现有效的受体占据，EC50 为 8 ng/g[2]。
GSK256471 (3-30 mg/kg，单次腹腔注射) 有效阻断中枢 NK3 受体功能，并抑制豚鼠的“湿狗抖”行为[2]。
GSK256471 (1-30 mg/kg，单次腹腔注射) 调节豚鼠大脑中脑边缘多巴胺系统的过度活跃，提示其作为抗精神病药物的潜力[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: "Wet dog shake" behavior model established in guinea pig[2]
Dosage: 3, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly inhibited behavior at 10 and 30 mg/kg.
Animal Model: Model of dopamine release in the nucleus accumbens established in guinea pig[2]
Dosage: 0.5, 1, 3, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly inhibited dopamine release at 1-10 mg/kg, but the effect disappeared at 30 mg/kg, presenting a "bell-shaped curve".
分子量

499.62

Formula

C29H29N3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GSK256471 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK2564711133706-08-7GSK 256471GSK-256471Neurokinin ReceptorNK receptorTachykinin receptorMicrodialysisDopaminergic neurotransmissionNucleus accumbensPrefrontal cortexGuinea pigTachykininPharmacokineticNon-surmountableInhibitorinhibitorinhibit

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