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BMY 7378

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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
Formula	C22H31N3O3.2HCl
CAS No.	21102-95-4
Storage	-20℃ for 3 years in powder form
Storage	-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
Synonyms	BMY 7378; BMY-7378; BMY7378.
SMILES Code	O=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 Vivo	BMY 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 model	Rat
Formulation & Dosage	Dissolved 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.

Purity ≥98%
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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.	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.	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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