B102
安非他酮 盐酸盐
≥98% (HPLC), solid, dopamine and norepinephrine transporter inhibitor
别名:
（±）-1-（3-氯苯基）-2-[（1,1-二甲基乙基）氨基]-1-丙酮 盐酸盐
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经验公式（希尔记法）:
C13H18ClNO · HCl
化学文摘社编号:
分子量:
276.20
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
250-759-9
MDL number:
产品名称
安非他酮 盐酸盐, ≥98% (HPLC), solid
InChI key
HEYVINCGKDONRU-UHFFFAOYSA-N
InChI
1S/C13H18ClNO.ClH/c1-9(15-13(2,3)4)12(16)10-6-5-7-11(14)8-10;/h5-9,15H,1-4H3;1H
SMILES string
Cl[H].CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1
description
Drug Control: Kábítószer / Narcotic Drug (Hungary), 78/2022. (XII. 28.) BM rendelet
assay
≥98% (HPLC)
form
solid
drug control
Kábítószer / Narcotic Drug (Hungary), 78/2022. (XII. 28.) BM rendelet
color
white
solubility
H2O: 15 mg/mL, clear
originator
GlaxoSmithKline
Quality Level
Gene Information
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), SLC6A2(6530), SLC6A3(6531)
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Application
Bupropion hydrochloride has been used as an anti-depressant and injected into mice intraperitoneally for forced swim test. It has also been used to study its effects on depression, anxiety and smoking cessation.
Biochem/physiol Actions
Bupropion possesses antidepressant and anxiolytic properties. It serves as a good auxiliary for people who makes an effort to give up smoking. It may also be used in the treatment for attention-deficit hyperactivity disorder.
Inhibits the dopamine and norepinephrine transporters with Kis of 2.8 μM and 1.4 μM, respectively. Does not inhibit the serotonin transporter (Ki = 45 μM). Antidepressant.
Features and Benefits
This compound is a featured product for ADME Tox and Neuroscience research. Discover more featured ADME Tox and Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Biogenic Amine Transporters page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
General description
Bupropion is structurally linked to the phenylethylamine family. It is a monocyclic aminoketone (chloropropiophenone).
Effects of bupropion on depression, anxiety and smoking cessation
Hernandez-Lozano M, et al.
Archives of Neuroscience, 15(4), 260-266 (2010)
Chronic ethanol potentiates the effect of neuropeptide s in the basolateral amygdala and shows increased anxiolytic and anti-depressive effects
Enquist J, et al.
Neuropsychopharmacology, 37(11), 2436-2436 (2012)
Jinhui Wang et al.
Frontiers in pharmacology, 11, 593518-593518 (2021-03-23)
Poziotinib is an orally active, irreversible, pan-HER tyrosine kinase inhibitor used to treat non-small cell lung cancer, breast cancer, and gastric cancer. Poziotinib is currently under clinical investigation, and understanding its drug-drug interactions is extremely important for its future development
B R Cooper et al.
The Journal of pharmacology and experimental therapeutics, 215(1), 127-134 (1980-10-01)
Bupropion (BW 323U; Wellbutrin), a novel compound with antidepressant effects in man, was found to reduce immobility in an "experimental helplessness" forced swimming antidepressant test in rats as did imipramine and amitriptyline. Higher doses produced elevated locomotor activity in an
Sonia M Grandi et al.
The Canadian journal of cardiology, 29(12), 1704-1711 (2013-11-26)
Smoking remains the most important modifiable risk factor for secondary prevention of cardiovascular events. We therefore performed a meta-analysis to determine the efficacy and safety of bupropion therapy started in-hospital for smoking cessation in patients with cardiovascular disease (CVD). We
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