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LOFEPRAMINE

LOFEPRAMINE Structure
LOFEPRAMINE
  • CAS No.23047-25-8
  • Chemical Name:LOFEPRAMINE
  • 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
  • FDA UNII OCA4JT7PAW
  • ATC code N06AA07
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H335-H413
  • Precautionary statements P261-P264-P273-P304+P340+P312-P403+P233-P501

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
LOFEPRAMINE Suppliers
Global(56)Suppliers
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LOFEPRAMINE Spectrum
23047-25-8, LOFEPRAMINERelated Search:
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Heterocycles
  • Aromatics
  • 抑制剂
  • FDA批准的配体
  • 神经系统用药
  • C26H27N2OCl
  • C26H27ClN2O
  • 洛非帕明,10 MM DMSO 溶液
  • 1-(4-氯苯基)-2-((3-(10,11-二氢-5H-二苯并[B,F]氮杂卓-5-基)丙基)(甲基)氨基)乙酮
  • LOFEPRAMINE,抑制剂
  • 洛非帕明
  • 氯苯酰丙咪嗪
  • 氯苯咪嗪
  • 23047-25-8
  • Lofepramine - Bio-X ?
  • Lofepramine, 10 mM in DMSO
  • Lofepramine in methanol
  • 2-[(3-{2-azatricyclo[9.4.0.03,?]pentadeca-1(11),3,5,7,12,14-hexaen-2-yl}propyl)(methyl)amino]-1-(4-chlorophenyl)ethan-1-one
  • Inhibitor,inhibit,Lofepramine
  • 1-(4-Chlorophenyl)-2-((3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)propyl)(methyl)amino)ethan-1-one
  • Ethanone, 1-(4-chlorophenyl)-2-[[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]methylamino]-
  • 1-(4-Chlorophenyl)-2-[[3-(10,11-dihydro-5H-dibenz(Z)[b,f]azepin-5-yl)propyl]methylamino]ethanone
  • Lopramine
  • Leo 640
  • Amplit
  • 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
  • Gamanil
  • LOFEPRAMINE

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