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BMY 7378
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMY 7378图片
CAS NO:21102-95-4
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)458.42
FormulaC22H31N3O3.2HCl
CAS No.21102-95-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 92 mg/mL (200.7 mM)
Water: 92 mg/mL (200.7 mM)
Ethanol: 20 mg/mL (43.6 mM)
Solubility (In vivo)Saline: 15 mg/mL
SynonymsBMY 7378; BMY-7378; BMY7378.
SMILES CodeO=C(N(CCN1CCN(C2=CC=CC=C2OC)CC1)C(C3)=O)CC43CCCC4.[H]Cl.[H]Cl
实验参考方法
In Vitro

In vitro activity: BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. BMY 7378 is selective for the α1D-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; rat α1d-adrenoceptor 8.2, human α1d-adrenoceptor 9.4 BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus.

In VivoBMY 7378 (pA2 of 8.67) is approximately 100 times more potent than yohimbine (pA2 of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA2 of 6.48) is approximately 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-adrenoceptor). BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats.
Animal modelRat
Formulation & DosageDissolved in 0.9% sodium chloride solution; 0.25-5 mg/kg; s.c. injection
References

Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41.