1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. BP 897

BP 897 是一种有效的部分多巴胺 D3 受体激动剂和弱 D2 受体拮抗剂。BP 897 在多巴胺 D3 受体 (Ki=0.92 nM) 上显示出高亲和力,而在 D2 受体上显示出 70 倍的低亲和力 (Ki=61 nM)。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 BP 897 hydrochloride 通常具有更好的水溶性和稳定性。

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BP 897 Chemical Structure

BP 897 Chemical Structure

CAS No. : 192384-87-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM)[1].

IC50 & Target

D2 Receptor

 

D3 Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
1.8 nM
Compound: BP-897
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
[PMID: 12361386]
CHO EC50
1.8 nM
Compound: 3a
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
[PMID: 16759104]
体外研究
(In Vitro)

BP 897 对 D1 和 D4 受体 (Ki=3 μM 和 0.3 μM)、α1 和 α2 肾上腺素能受体 (Ki=60 nM 和 83 nM) 和 5HT1A 和 5HT7 受体 (Ki=84 nM 和 345 nM) 具有亲和力;对毒蕈碱型受体、组胺受体和阿片受体的亲和力则忽略不计 (Ki>1 μM)[1]
在表达人 D3 受体的 NG 108-15 细胞中,BP 897 抑制毛喉素诱导的环 AMP 积累,EC50=1 nM。BP 897 激活有丝分裂发生,这种反应优先被 D3 受体拮抗剂 Nafadotride (1 μM) 拮抗。BP 897 也部分拮抗 quinpirole (10 nM) 诱导的反应[1]

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

体内研究
(In Vivo)
Animal Model: Male Listar hooded rats[1]
Dosage: 0.05, 0.5, 1 mg/kg
Administration: i.p.; 30 min before the session
Result: Reduced cocaine-seeking behaviour before the first infusion of cocaine, in a dose-dependent manner, at doses similar to those at which BP 897 produced its responses on rotations and c-fos expression.
分子量

417.54

Formula

C26H31N3O2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
BP 897
目录号:
HY-114085
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