BMY 7378

Alias: BMY 7378; BMY-7378; BMY7378
Cat No.:V0987 Purity: ≥98%
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.
BMY 7378 Chemical Structure CAS No.: 21102-95-4
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of BMY 7378:

  • BMY-7378 HCl (BMY73)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT1A ( pIC50 = 8.3 ); α1D-adrenoceptor ( pKi = 8.2 ); Dopamine D2 receptor ( pIC50 = 7.4 ); α2C-adrenoceptor ( pKi = 6.54 ); 5-HT1C ( pIC50 = 6.4 )
ln Vitro

In vitro activity: BMY 7378 exhibits selectivity for the alpha 1D-adrenoceptor subtype (pKi: hamster alpha 1b-adrenoceptor 6.2, human alpha 1b-adrenoceptor 7.2; bovine alpha 1c-adrenoceptor 6.1, human alpha 1c-adrenoceptor 6.6; rat alpha 1d-adrenoceptor 8.2, human alpha 1d-adrenoceptor 9.4) and exhibits a high affinity (pA2, 8.9) for rat aorta alpha 1-adrenoceptor][2].

ln 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 Protocol
Dissolved in 0.9% sodium chloride solution; 0.25-5 mg/kg; s.c. injection
Rat
References

[1]. The specific contribution of the novel alpha-1D adrenoceptor to the contraction of vascular smooth muscle. J Pharmacol Exp Ther. 1995;275(3):1583-1589.

[2]. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1995;272(2-3):R5-R6.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H33CL2N3O3
Molecular Weight
458.42
Exact Mass
457.19
CAS #
21102-95-4
Related CAS #
21102-94-3 (Free base); 21102-95-4 (HCl)
SMILES
COC1=CC=CC=C1N2CCN(CC2)CCN3C(=O)CC4(CCCC4)CC3=O.Cl.Cl
InChi Key
NIBOMXUDFLRHRV-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H31N3O3.2ClH/c1-28-19-7-3-2-6-18(19)24-13-10-23(11-14-24)12-15-25-20(26)16-22(17-21(25)27)8-4-5-9-22;;/h2-3,6-7H,4-5,8-17H2,1H3;2*1H
Chemical Name
8-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-8-azaspiro[4.5]decane-7,9-dione;dihydrochloride
Synonyms
BMY 7378; BMY-7378; BMY7378
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1814 mL 10.9070 mL 21.8141 mL
5 mM 0.4363 mL 2.1814 mL 4.3628 mL
10 mM 0.2181 mL 1.0907 mL 2.1814 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
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