BMY 7378 | BMY 7378 Dihydrochloride | α1D-AR Antagonist

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

货号：A529649 同义名： BMY 7378 Dihydrochloride

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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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5-羟色胺受体亚型比较
肾上腺素能受体亚型比较

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								98%
Lamotrigine	+ 5-HT (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM								98%
Venlafaxine	✔								98%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								98%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	98%
Fluoxetine HCl	✔								99.5%
Paroxetine hydrochloride	✔							AChR	97%
BMY 7378		++ 5-HT1D, pIC50: 5.9 5-HT1A, pIC50: 6.4	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						98% HPLC
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM						99%+
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 nM						99%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						99%+
Sarpogrelate HCl			++++ 5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					98%
VUF10166				++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
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		97%
Risperidone		++ 5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1B, pKi: 6.1 5-HT1D, pKi: 6	++ 5-HT2B, pKi: 6.2 5-HT2A, pKi: 6.6			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
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 ↓ ↑	纯度
Ivabradine HCl	✔			98%
Maprotiline hydrochloride	✔			98%
Cisatracurium besylate	✔			98%
Yohimbine HCI		✔		99+%
BMY 7378		++ α1D-adrenoceptor, pKi: 5.1 α2C-adrenoceptor, pKi: 6.54	+ β1-adrenoceptor, pIC50: 5.1	97%
Asenapine maleate		++++ α2A-adrenergic receptor, pKi: 8.9 α2B-adrenergic receptor, pKi: 8.9		97%
Piribedil		++ adrenoceptor α2C, pKi: 7.2 adrenoceptor α2A, pKi: 7.1		98%
Prazosin HCl		✔		95%
Silodosin		✔		98%
Phenoxybenzamine HCl		✔		98%
Naftopidil		+++ α1A-adrenergic receptor, Ki: 3.7 nM α1D-adrenergic receptor, Ki: 20 nM		98%
Naftopidil 2HCl		+ α1-adrenergic receptor, IC50: 0.2 μM		97%
Alfuzosin HCl		✔		98%
Terazosin HCl		✔		99%
Atipamezole		✔		95%
Phentolamine methanesulfonate salt		✔		99%
Doxazosin mesylate		✔		98%
Tolazoline HCl		✔		98%
Zenidolol hydrochloride			++++ β1-adrenergic receptor, Ki: 611nM β2-adrenergic receptor, Ki: 0.7nM	98%
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

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

动物实验配方

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

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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

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

BMY 7378 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

BMY 7378 质控信息

BMY 7378 生物活性

BMY 7378 参考文献

BMY 7378 实验方案

BMY 7378 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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BMY 7378 纯度/质量文件产品仅供科研