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BMY 7378 Dihydrochloride 5-HT Receptor antagonist

Name: BMY 7378 Dihydrochloride
Brand: Selleck Chemicals
SKU: S2691
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S2691

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

Chemical Structure

Molecular Weight: 458.42

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.13

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Chemical Information, Storage & Stability

Molecular Weight	458.42	Formula	C₂₂H₃₁N₃O₃.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	21102-95-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=CC=CC=C1N2CCN(CC2)CCN3C(=O)CC4(CCCC4)CC3=O.Cl.Cl

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	15.000mg/ml (32.72mM)	Taking the 1 mL working solution as an example, add 15 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-HT1A ^[2] 8.3(pIC50) α1D-adrenoceptor ^[2] 8.2(pKi) Dopamine D2 receptor ^[2] 7.4(pIC50) α2C-adrenoceptor ^[1] 6.54(pKi) 5-HT1C ^[2] 6.4(pIC50) 5-HT1D ^[2] 5.9(pIC50) H1 receptor ^[2] 5.7(pIC50) 5-HT2 ^[2] 5.5(pIC50) H2 receptor ^[2] 5.3(pIC50) α2-adrenoceptor ^[2] 5.1(pIC50) β1-adrenoceptor ^[2] 5.1(pIC50) Dopamine D1 receptor ^[2] 5(pIC50)
In vitro	BMY 7378 shows 10-fold selectivity for α_2C-adrenoceptors over other α₂-adrenoceptors with pKi of 6.54. ^[1] BMY 7378 is selective for the α_1D-adrenoceptor subtype (PKi: hamster α_1b-adrenoceptor 6.2, human α_1b-adrenoceptor 7.2; bovine α_1c-adrenoceptor 6.1, human α_1c-adrenoceptor 6.6; rat α_1d-adrenoceptor 8.2, human α_1d-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	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 (α_2C-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]
References	https://pubmed.ncbi.nlm.nih.gov/16176444/ https://pubmed.ncbi.nlm.nih.gov/7713154/ https://pubmed.ncbi.nlm.nih.gov/1535319/ https://pubmed.ncbi.nlm.nih.gov/1970304/

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