LOFEPRAMINE
- Product Name
- LOFEPRAMINE
- CAS No.
- 23047-25-8
- Chemical Name
- LOFEPRAMINE
- Synonyms
- Amplit;Gamanil;Leo 640;Lopramine;LOFEPRAMINE;Lofepramine in methanol;Inhibitor,inhibit,Lofepramine;4'-Chloro-2-[[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl-methylamino]acetophenone;1-(4-Chlorophenyl)-2-[[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]methylamino]ethanone;Ethanone, 1-(4-chlorophenyl)-2-[[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]methylamino]-
- CBNumber
- CB7799244
- Molecular Formula
- C26H27ClN2O
- Formula Weight
- 418.96
- MOL File
- 23047-25-8.mol
LOFEPRAMINE Property
- Melting point:
- 103-105°C
- vapor pressure
- 0Pa at 25℃
- storage temp.
- Store at +4°C
- solubility
- Chloroform (Slightly), Methanol (Slightly)
- form
- Solid
- color
- Light Yellow to Light Beige
- Water Solubility
- 2.04mg/L at 25℃
- Stability:
- Unstable in Solution
Safety
- Hazardous Substances Data
- 23047-25-8(Hazardous Substances Data)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H335May cause respiratory irritation
H413May cause long lasting harmful effects to aquatic life
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P273Avoid release to the environment.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 20813
- Product name
- Lofepramine
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 20813
- Product name
- Lofepramine
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- 20813
- Product name
- Lofepramine
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 20813
- Product name
- Lofepramine
- Purity
- ≥95%
- Packaging
- 50mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- 2545
- Product name
- Lofepramine
- Purity
- ≥99%(HPLC)
- Packaging
- 50
- Price
- $605
- Updated
- 2021/12/16
LOFEPRAMINE Chemical Properties,Usage,Production
Description
Lofepramine is a first generation tricyclic antidepressant that is extensively metabolized to desipramine. It potently inhibits serotonin and norepinephrine transporters (Kds = 70 and 5.4 nM, respectively) and less potently antagonizes serotonin, histamine, and muscarinic receptors.
Chemical Properties
Light Yellow Solid
Originator
Gamonil,E. Merck
Uses
Psychotropic drug related to imipramine. Antidepressant.
Definition
ChEBI: Lofepramine is a dibenzoazepine, a member of monochlorobenzenes, a tertiary amino compound and an aromatic ketone. It has a role as an antidepressant.
Manufacturing Process
9.8 parts of 10,11-dihydro-5H-dibenzo[b,f]azepine are dissolved in 10 parts of
dry toluene and 3.1 parts of sodium amide are added and the mixture is
refluxed and stirred for four hours. A solution of 13.5 parts of 1-(4-
chlorophenyl)-2-[(3-chloropropyl)methylamino]ethanone in 20 parts of dry
toluene is added dropwise and the mixture is stirred and refluxed for eight
hours.
After cooling to room temperature water is carefully added to the reaction
mixture and the toluene solution is extracted with water to which hydrochloric
acid is added so that the aqueous phase obtains the pH-value of 5. The
aqueous extract is discarded and the toluene phase is evaporated to dryness
in vacuum. The residue is dissolved in 50 parts of methanol. Hydrogen gas is
introduced to give the crystalline hydrochloride 1-(4-chlorophenyl)-2-((3-
(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)propyl)methylamino)ethanone;
MP: 154°-156°C. The hydrochloride may be removed by adding an equivalent
of any base (triethyl amine, sodium hydroxide and so on).
Therapeutic Function
Antidepressant
Biological Activity
Serotonin and noradrenalin re-uptake inhibitor (SNRI) that is metabolized to desipramine. Produces inhibition of liver tryptophan pyrollase activity in vitro and displays antidepressant properties in vivo .
Mechanism of action
Lofepramine differs from imipramine by the attachment of a p-chlorophenacyl moiety to the N-aminopropyl side chain. This change confers enhanced lipophilicity and the potential of more rapid distribution into the CNS with greater in vitro affinity and selectivity for NET. Its mechanism of antidepressant action is attributed to its rapid metabolism to the secondary amine metabolite, desipramine, which selectively inhibits the neuronal uptake of NE.
LOFEPRAMINE Preparation Products And Raw materials
Raw materials
Preparation Products
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