Lensiprazine - CAS 327026-93-7
Catalog number: 327026-93-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H27FN4O2
Molecular Weight:
422.50
COA:
Inquire
Targets:
Dopamine Receptor
Description:
Lensiprazine is a potent in vitro dopamine receptor antagonist and highly active as serotonin reuptake inhibitor.
Purity:
≥98%
Appearance:
Solid powder
Synonyms:
SLV-314; SLV 314; SLV314; (2R)-8-[4-[3-(5-Fluoro-1H-indol-3-yl)propyl]-1-piperazinyl]-2-methyl-2H-1,4-benzoxazin-3(4H)-one
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
D(2) receptor antagonist
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
Density:
1.262
InChIKey:
SDAMYSWGWHXMRT-MRXNPFEDSA-N
InChI:
1S/C24H27FN4O2/c1-16-24(30)27-21-5-2-6-22(23(21)31-16)29-12-10-28(11-13-29)9-3-4-17-15-26-20-8-7-18(25)14-19(17)20/h2,5-8,14-16,26H,3-4,9-13H2,1H3,(H,27,30)/t16-/m1/s1
Canonical SMILES:
CC1C(=O)NC2=C(O1)C(=CC=C2)N3CCN(CC3)CCCC4=CNC5=C4C=C(C=C5)F
Current Developer:
Solvay
1.Metabolic disposition of enciprazine, a non-benzodiazepine anxiolytic drug, in rat, dog and man.
Scatina JA1, Lockhead SR, Cayen MN, Sisenwine SF. Xenobiotica. 1991 Dec;21(12):1591-604.
1. The excretion and metabolism of enciprazine, an anxiolytic drug, was examined in rat, dog and man. 2. In rats and dogs that received 14C-enciprazine dihydrochloride orally and by i.v. injection, the drug was well absorbed. Radioactivity was excreted predominantly in the faeces of rats, equally in urine and faeces of dogs, and to a major extent in human urine. 3. Metabolic profiles, which were evaluated in urine and in rat bile, were similar following oral and i.v. dosing to rats and dogs. 4. Unchanged drug was not detected in rat, dog or human excreta. Glucuronide conjugates of 4-hydroxyenciprazine, m-desmethylenciprazine, p-desmethylenciprazine and enciprazine were detected in the excreta of all three species. A glycol metabolite was present only in rat bile and human urine. A metabolite desmethylated in the phenyl ring of the phenylpiperazine moiety also appeared to be present only in human urine. 5. Structural confirmation of the major metabolites in human urine and rat bile was accomplished by h.
2.Pilot study on the therapeutic efficacy, clinical safety, and dosage finding of enciprazine in out-patients with anxious and anxious-depressive syndromes.
Scheibe G1, Grohmann R, Buchheim P. Arzneimittelforschung. 1990 Jun;40(6):644-6.
The new basic propanolamine derivative enciprazine (D 13 112) was tested in an open single-blind phase-II trial with regard to therapeutic efficacy, clinical safety, and dosage finding. The drug showed a good efficacy in mildly ill patients. Under the highest dosage frequently fatigue was reported. In 78% of the patients the enciprazine trial succeeded in shifting patients from benzodiazepines to non-benzodiazepines or in discontinuation of psychopharmacotherapy after completion of the trial.
3.Comparison of changes in the EEG of freely moving rats induced by enciprazine, buspirone and diazepam.
Nickel B1, Szelenyi I. Neuropharmacology. 1989 Aug;28(8):799-803.
The effect of enciprazine, buspirone and diazepam was investigated on the cortical electrical activity in freely-moving rats. Enciprazine (5 mg/kg, i.p.) and buspirone (5 mg/kg, i.p.) induced comparable changes, consisting in decreases of mean power values in delta and theta and increases in alpha and beta EEG frequency bands. Regarding only a particular area of the brain or particular frequency bands, these two compounds could not be clearly separated from each other. Changes in frequency bands induced by O-methoxy-phenyl-piperazine (5 mg/kg i.p.) (D 15157), the presumed main metabolite of enciprazine, were dose-related to that caused by the parent compound. The second metabolite (R,S)-1-4-(1-methoxy-4-hydroxy-phenyl)piperazin-1-yl-3-(3,4,5- trimethoxyphenoxy)propan-2-ol-dihydrochloride (D 20092) (5 mg/kg i.p.) evoked only minimal changes in the different frequency bands of the rats. The power spectra did not significantly differ from those seen in animals treated with saline.
4.Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
Engel J1, Fleischhauer I, Jakovlev V, Kleemann A, Kutscher B, Nickel B, Rauer H, Werner U, Szelenyi I, Johanson CE, et al. J Med Chem. 1990 Nov;33(11):2976-81.
In the course of studies on tranquilizers, new non-benzodiazepine-like compounds were synthesized. These are 1-(3,4,5-trimethoxyphenoxy)-3-[4-(2-methoxyphenyl)piperazinyl]prop an-2-ol (INN: enciprazine) and derivatives thereof which were screened pharmacologically in order to evaluate their central nervous system activity. Compounds with marked antiaggressive and anxiolytic properties but without dependence potential could be detected. Enciprazine was selected for clinical investigations.
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CAS 327026-93-7 Lensiprazine

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