1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor 5-HT Receptor
  3. BMY 7378

BMY 7378 是 α1D 肾上腺素受体 1D-AR) 的选择性拮抗剂。BMY 7378 与表达克隆大鼠 α1D-AR 的膜结合的亲和力 (Ki=2 nM) 高于与克隆大鼠 α1A-AR (Ki=800 nM) 或仓鼠 α1B-AR (Ki=600 nM) 结合的亲和力 >100 倍。BMY 7378 是一种 5-HT1A 受体部分激动剂。

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BMY 7378 Chemical Structure

BMY 7378 Chemical Structure

CAS No. : 21102-95-4

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  • 生物活性

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生物活性

BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist[1][2].

IC50 & Target[1]

rat α1A-adrenergic receptor

800 nM (Ki)

hamster alpha1B-adrenergic receptor

600 nM (Ki)

rat alpha1D-adrenergic receptor

2 nM (Ki)

5-HT1A Receptor

 

体外研究
(In Vitro)

BMY 7378 is selective for the alpha 1D-adrenoceptor subtype (pKi: hamster alpha 1b-adrenoceptor 6.2, human alpha 1b-adrenoceptor 7.2; bovine alpha 1c-adrenoceptor 6.1, human alpha 1c-adrenoceptor 6.6; rat alpha 1d-adrenoceptor 8.2, human alpha 1d-adrenoceptor 9.4) and has high affinity (pA2, 8.9) for rat aorta alpha 1-adrenoceptor[2].

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

分子量

458.42

Formula

C22H33Cl2N3O3

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
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  • 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:
BMY 7378
目录号:
HY-100554
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