Home Neuronal Signaling 5-HT Receptor antagonist - Adrenergic Receptor antagonist BMY 7378 Dihydrochloride For research use only.

BMY 7378 Dihydrochloride

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

BMY 7378 Dihydrochloride Chemical Structure

BMY 7378 Dihydrochloride Chemical Structure

CAS No. 21102-95-4

Purity & Quality Control

Batch: S269101 DMSO]92 mg/mL]false]Water]92 mg/mL]false]Ethanol]20 mg/mL]false Purity: 99.13%
99.13

BMY 7378 Dihydrochloride Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
Targets
5-HT1A [2] α1D-adrenoceptor [2] Dopamine D2 receptor [2] α2C-adrenoceptor [1] 5-HT1C [2] Click to View More Targets
8.3(pIC50) 8.2(pKi) 7.4(pIC50) 6.54(pKi) 6.4(pIC50)
In vitro
In vitro BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. [1] 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 [2] BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. [3]
In Vivo
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).[1] 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. [4]
Animal Research Animal Models rats
Dosages 0.25-5 mg/kg
Administration Inject subcutaneously at a single dose

Chemical Information & Solubility

Molecular Weight 458.42 Formula

C22H31N3O3.2HCl
CAS No. 21102-95-4 SDF Download BMY 7378 Dihydrochloride SDF
Smiles COC1=CC=CC=C1N2CCN(CC2)CCN3C(=O)CC4(CCCC4)CC3=O.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (200.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 92 mg/mL

Ethanol : 20 mg/mL


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