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BMY 7378 {[allProObj[0].p_purity_real_show]}

货号：A529649 同义名： BMY 7378 Dihydrochloride Ambeed 开学季，买赠积分，赢豪礼

BMY 7378 2HCl is a 5-HT1A partial agonist and a high-affinity α1D adrenoceptor antagonist with Ki values of 2, 800 and 600 nM for cloned rat α1D, rat α1A and hamster α1B receptors respectively.

BMY 7378 化学结构 CAS号：21102-95-4
BMY 7378 化学结构
CAS号：21102-95-4
BMY 7378 3D分子结构
CAS号：21102-95-4
BMY 7378 化学结构 CAS号：21102-95-4
BMY 7378 3D分子结构 CAS号：21102-95-4
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BMY 7378 纯度/质量文件 产品仅供科研

货号：A529649 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		{[allProObj[0].p_purity_real_show]}
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		{[allProObj[0].p_purity_real_show]}
Venlafaxine ✔ {[allProObj[0].p_purity_real_show]}
Fluvoxamine maleate ✔ {[allProObj[0].p_purity_real_show]}
Iloperidone ✔ {[allProObj[0].p_purity_real_show]}
Ziprasidone HCl ✔ {[allProObj[0].p_purity_real_show]}
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		{[allProObj[0].p_purity_real_show]}
Dapoxetine HCl ✔ {[allProObj[0].p_purity_real_show]}
Trazodone ✔ {[allProObj[0].p_purity_real_show]}
Clomipramine HCl ✔ {[allProObj[0].p_purity_real_show]}
Mirtazapine ✔ {[allProObj[0].p_purity_real_show]}
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		{[allProObj[0].p_purity_real_show]}
Duloxetine ✔ {[allProObj[0].p_purity_real_show]}
Sertraline HCl ++

5-HT, Ki: 13 nM

 		{[allProObj[0].p_purity_real_show]}
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		{[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl ✔ GluR {[allProObj[0].p_purity_real_show]}
Fluoxetine HCl ✔ {[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride ✔ AChR {[allProObj[0].p_purity_real_show]}
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		{[allProObj[0].p_purity_real_show]}
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		{[allProObj[0].p_purity_real_show]}
LY310762 +

5-HT1D, Ki: 249 nM

 		{[allProObj[0].p_purity_real_show]}
Cyclobenzaprine HCI ✔ {[allProObj[0].p_purity_real_show]}
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		{[allProObj[0].p_purity_real_show]}
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		{[allProObj[0].p_purity_real_show]}
Olanzapine ✔ {[allProObj[0].p_purity_real_show]}
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		{[allProObj[0].p_purity_real_show]}
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		{[allProObj[0].p_purity_real_show]}
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		{[allProObj[0].p_purity_real_show]}
Agomelatine ✔ {[allProObj[0].p_purity_real_show]}
Clozapine ✔ {[allProObj[0].p_purity_real_show]}
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT {[allProObj[0].p_purity_real_show]}
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		{[allProObj[0].p_purity_real_show]}
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		{[allProObj[0].p_purity_real_show]}
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		{[allProObj[0].p_purity_real_show]}
Tropisetron ✔ {[allProObj[0].p_purity_real_show]}
Palonosetron ✔ {[allProObj[0].p_purity_real_show]}
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		{[allProObj[0].p_purity_real_show]}
Ondansetron ✔ {[allProObj[0].p_purity_real_show]}
Granisetron ✔ {[allProObj[0].p_purity_real_show]}
Alosetron HCl ✔ {[allProObj[0].p_purity_real_show]}
Ondansetron hydrochloride dihydrate ✔ {[allProObj[0].p_purity_real_show]}
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		{[allProObj[0].p_purity_real_show]}
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		{[allProObj[0].p_purity_real_show]}
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		{[allProObj[0].p_purity_real_show]}
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		{[allProObj[0].p_purity_real_show]}
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		{[allProObj[0].p_purity_real_show]}
Intepirdine ++++

5-HT6, pKi: 9.63

 		{[allProObj[0].p_purity_real_show]}
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		{[allProObj[0].p_purity_real_show]}
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ {[allProObj[0].p_purity_real_show]}
Maprotiline hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Cisatracurium besylate ✔ {[allProObj[0].p_purity_real_show]}
Yohimbine HCI ✔ {[allProObj[0].p_purity_real_show]}
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

 		+

β1-adrenoceptor, pIC50: 5.1

 		{[allProObj[0].p_purity_real_show]}
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

 		{[allProObj[0].p_purity_real_show]}
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

 		{[allProObj[0].p_purity_real_show]}
Prazosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Silodosin ✔ {[allProObj[0].p_purity_real_show]}
Phenoxybenzamine HCl ✔ {[allProObj[0].p_purity_real_show]}
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

 		{[allProObj[0].p_purity_real_show]}
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		{[allProObj[0].p_purity_real_show]}
Alfuzosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Terazosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Atipamezole ✔ {[allProObj[0].p_purity_real_show]}
Phentolamine methanesulfonate salt ✔ {[allProObj[0].p_purity_real_show]}
Doxazosin mesylate ✔ {[allProObj[0].p_purity_real_show]}
Tolazoline HCl ✔ {[allProObj[0].p_purity_real_show]}
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

BMY 7378 生物活性

靶点

  • α-adrenergic receptor

    α1D-adrenoceptor, pKi:5.1

    α2C-adrenoceptor, pKi:6.54

  • β-adrenergic receptor

    β1-adrenoceptor, pIC50:5.1

  • 5-HT2

    5-HT2, pIC50:5.5

  • 5-HT1

    5-HT1D, pIC50:5.9

    5-HT1A, pIC50:6.4
描述 BMY 7378 Dihydrochloride is a multi-target inhibitor, which acts on α 2C and α 1D adrenoceptors, with PKI of 6.54 and 8.2, respectively. It is a mixed 5-HT1A receptor agonist and antagonist, with PKI of 8.3[3]. In vitro research suggests that BMY 7378 Dihydrochloride has a PKI value 6.06±0.09 in AC01 cells[4]. In vivo , BMY 7378 Dihydrochloride dose-dependently (0.25-5 mg/kg) decreased 8-OH-DPAT (0.75 mg/kg)-induced unmeasured level of forepaw stampede and head shaking in rats. In the ventral hippocampus of anesthetized rats, BMY 7378 Dihydrochloride significantly reduced the release of 5-HT in a dose-dependent manner by microdialysis[5].

BMY 7378 参考文献

[1]Cleary L, et al. Auton Autacoid Pharmacol, 2005, 25(4), 135-141.

[2]Goetz AS, et al. Eur J Pharmacol, 1995, 272(2-3), R5-6.

[3]Yang HT, Endoh M. Pharmacological evidence for alpha(1D)-adrenoceptors in the rabbit ventricular myocardium: analysis with BMY 7378. Br J Pharmacol. 1997 Dec;122(8):1541-50. doi: 10.1038/sj.bjp.0701506. PMID: 9422797; PMCID: PMC1565100.

[4]Ohmi K, Shinoura H, Nakayama Y, Goda N, Tsujimoto G. Characterization of alpha 1-adrenoceptors expressed in a novel vascular smooth muscle cell line cloned from p53 knockout mice, P53LMAC01 (AC01) cells. Br J Pharmacol. 1999 Jun;127(3):756-62. doi: 10.1038/sj.bjp.0702588. PMID: 10401567; PMCID: PMC1566058.

[5]O'Connor JJ, Rowan MJ, Anwyl R. Actions of 5-HT1 ligands on excitatory synaptic transmission in the hippocampus of alert rats. Br J Pharmacol. 1990 Sep;101(1):171-7. doi: 10.1111/j.1476-5381.1990.tb12108.x. PMID: 1980835; PMCID: PMC1917630.

BMY 7378 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.91mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL

BMY 7378 技术信息

CAS号21102-95-4
分子式C22H33Cl2N3O3
分子量 458.422
别名 BMY 7378 Dihydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度
动物实验配方

Tags: BMY 7378 | 21102-95-4 | BMY7378 | BMY-7378 | α1D-AR Antagonist | GPCR/G Protein | Neuronal Signaling | Adrenergic Receptor | 5-HT Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | BMY 7378 纯度/质量文件 | BMY 7378 亚型比较 | BMY 7378 生物活性 | BMY 7378 参考文献 | BMY 7378 实验方案 | BMY 7378 技术信息

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