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BMY 7378

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Chemical Structure| 21102-95-4 同义名 : BMY 7378 Dihydrochloride
CAS号 : 21102-95-4
货号 : A529649
分子式 : C22H33Cl2N3O3
纯度 : 97%
分子量 : 458.422
MDL号 : MFCD00153771
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：
生物活性
靶点

  • α-adrenergic receptor

    α2C-adrenoceptor, pKi:6.54

    α1D-adrenoceptor, pKi:5.1

  • β-adrenergic receptor

    β1-adrenoceptor, pIC50:5.1

  • 5-HT2

    5-HT2, pIC50:5.5

  • 5-HT1

    5-HT1A, pIC50:6.4

    5-HT1D, pIC50:5.9
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].
实验方案
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
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.