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      BMY 7378
      BMY 7378

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0987
      CAS #: 21102-95-4Purity ≥98%

      Description: BMY 7378 (BMY-7378; BMY7378) is a multi-target compound that inhibits α2C-adrenoceptor and α1D-adrenoceptor with pKi values of 6.54 and 8.2, respectively.

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

      Related CAS #: 21102-94-3 (free base); 21102-95-4 (HCl)

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      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


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      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. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

       
      BMY 7378
      Effects of BMY 7378 and prazosin (PZ) on concentration–contraction curves for phenylephrine (PE) in rat carotid artery rings. Br J Pharmacol. 2001 Apr; 132(8): 1852–1858.
      		 
      BMY 7378
      Double peaked vasoconstrictor responses to periarterial electrical nerve stimulation and the effects of BMY 7378, CEC and αβ-m ATP in an isolated, perfused canine splenic artery. Br J Pharmacol. 2001 Apr; 132(8): 1852–1858.
      		 
      BMY 7378
      Effect of BMY 7378, 5-methylurapidil and (+)-cyclazocine on chloroethylclonidine-induced contraction in aorta from spontaneously hypertensive rats. Br J Pharmacol. 2001 Apr; 132(8): 1

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