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Referencia número: HY-137107

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Radafaxine

(Synonyms: (S,S)-Hydroxybupropion; GW-353162A free base; BW-306U free base)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Radafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion.

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No. CAS: 192374-14-4
Fòrmula: C₁₃H₁₈ClNO₂
Peso molecular:255.74

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

Radafaxine Chemical Structure

No. CAS: 192374-14-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Publications (1)
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Actividad biológica

Descripciòn

Radafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>100 μM Compound: (2S,3S)-4a	Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells after 90 mins by scintillation counting Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells after 90 mins by scintillation counting	[PMID: 20509659]
HEK293	IC₅₀	>100 μM Compound: (2S,3S)-4a	Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells after 90 mins by scintillation counting Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells after 90 mins by scintillation counting	[PMID: 20509659]
HEK293	IC₅₀	100 nM Compound: (S,S)-5a	Inhibition of human NET in HEK293 cells assessed as inhibition of [3H]norepinephrine uptake Inhibition of human NET in HEK293 cells assessed as inhibition of [3H]norepinephrine uptake	[PMID: 21319801]
HEK293	IC₅₀	20 μM Compound: (S,S)-5a	Antagonist activity at human alpha4beta2 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux Antagonist activity at human alpha4beta2 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux	[PMID: 21319801]
HEK293	IC₅₀	220 nM Compound: (S,S)-5a	Inhibition of human DAT in HEK293 cells assessed as inhibition of [3H]dopamine uptake Inhibition of human DAT in HEK293 cells assessed as inhibition of [3H]dopamine uptake	[PMID: 21319801]
HEK293	IC₅₀	3.3 μM Compound: (S,S)-5a	Antagonist activity at human alpha3beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux Antagonist activity at human alpha3beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux	[PMID: 21319801]
HEK293	IC₅₀	30 μM Compound: (S,S)-5a	Antagonist activity at human alpha4beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux Antagonist activity at human alpha4beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux	[PMID: 21319801]
HEK293	IC₅₀	387 nM Compound: (S,S)-5a	Inhibition of human SERT in HEK293 cells assessed as inhibition of [3H]serotonin uptake Inhibition of human SERT in HEK293 cells assessed as inhibition of [3H]serotonin uptake	[PMID: 21319801]
HEK293	IC₅₀	9900 nM Compound: (2S,3S)-4a	Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells after 90 mins by scintillation counting Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells after 90 mins by scintillation counting	[PMID: 20509659]
SH-SY5Y	IC₅₀	6.5 μM Compound: (2S,3S)-4a	Antagonist activity at alpha3beta4 nicotinic receptor in human SH-SY5Y cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting Antagonist activity at alpha3beta4 nicotinic receptor in human SH-SY5Y cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting	[PMID: 20509659]
TE-671	IC₅₀	7.6 μM Compound: (2S,3S)-4a	Antagonist activity at alpha-1-beta-1-gamma-delta nicotinic receptor in human TE671 cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting Antagonist activity at alpha-1-beta-1-gamma-delta nicotinic receptor in human TE671 cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting	[PMID: 20509659]

Chemical Information

No. CAS 192374-14-4
Peso molecular 255.74
Fòrmula C₁₃H₁₈ClNO₂
SMILES

O[C@]1(C2=CC=CC(Cl)=C2)[C@H](C)NC(C)(C)CO1
Synonyms

(S,S)-Hydroxybupropion; GW-353162A free base; BW-306U free base
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Journal Impact Factor

Nature

Substrate binding and inhibition mechanism of norepinephrine transporter. [Abstract]

2024 Sep;633(8029):473-479. PMID: 39143211

Pureza y Documentación

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Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Volkow ND, et al. The slow and long-lasting blockade of dopamine transporters in human brain induced by the new antidepressant drug radafaxine predict poor reinforcing effects. Biol Psychiatry. 2005 Mar 15;57(6):640-6. [Content Brief]

[2]. Xu H, et al. Stereoselective analysis of hydroxybupropion and application to drug interaction studies. Chirality. 2007 Mar;19(3):163-70. [Content Brief]

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Keywords

Radafaxine

1 Cited Publications

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Radafaxine

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