1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Adrenergic Receptor
  3. Nefazodone hydrochloride

Nefazodone hydrochloride (Synonyms: BMY-13754; MJ-13754-1)

Cat. No.: HY-B1396 Purity: 99.02%
Handling Instructions

Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.

For research use only. We do not sell to patients.

Nefazodone hydrochloride Chemical Structure

Nefazodone hydrochloride Chemical Structure

CAS No. : 82752-99-6

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10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
Estimated Time of Arrival: December 31
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Description

Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

IC50 & Target

5-HT2A Receptor

5.8 nM (Ki)

α1-adrenergic receptor

 

In Vitro

Nefazodone hydrochloride (BMY-13754) is a phenylpiperazine antidepressant with a mechanism of action that is distinct from those of other currently available drugs. Nefazodone hydrochloride potently and selectively blocks postsynaptic serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A receptors and moderately inhibits serotonin and noradrenaline (norepinephrine) reuptake. Nefazodone hydrochloride is also an inhibitor of the hepatic P-450 isoenzyme CYP3A4[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

506.47

Formula

C₂₅H₃₃Cl₂N₅O₂

CAS No.

82752-99-6

SMILES

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)N=C(CC)N1CCOC4=CC=CC=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (98.72 mM; Need ultrasonic)

H2O : 2 mg/mL (3.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9745 mL 9.8723 mL 19.7445 mL
5 mM 0.3949 mL 1.9745 mL 3.9489 mL
10 mM 0.1974 mL 0.9872 mL 1.9745 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NefazodoneBMY-13754 MJ-13754-1BMY13754BMY 137545-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorantidepressantpostsynapticnorepinephrinereuptaketransporterInhibitorinhibitorinhibit

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Product Name:
Nefazodone hydrochloride
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HY-B1396
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