| Bioactivity | 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]. |
| Invitro | 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]. |
| Name | Nefazodone hydrochloride |
| CAS | 82752-99-6 |
| Formula | C25H33Cl2N5O2 |
| Molar Mass | 506.47 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Pullar IA, et al. LY367265, an inhibitor of the 5-hydroxytryptamine transporter and 5-hydroxytryptamine(2A) receptor antagonist: a comparison with the antidepressant, nefazodone. Eur J Pharmacol. 2000;407(1-2):39-46. [2]. Ellingrod VL, et al. Nefazodone: a new antidepressant. Am J Health Syst Pharm. 1995;52(24):2799-2812. |
Nefazodone hydrochloride
CAS: 82752-99-6 F: C25H33Cl2N5O2 W: 506.47
Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of
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