Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C16H23BrN2O3.ClH |
| Molecular Weight | 407.73 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCN1CCC[C@H]1CNC(=O)C2=C(OC)C(Br)=CC=C2OC
InChI
InChIKey=WCPXLMIPGMFZMY-MERQFXBCSA-N
InChI=1S/C16H23BrN2O3.ClH/c1-4-19-9-5-6-11(19)10-18-16(20)14-13(21-2)8-7-12(17)15(14)22-3;/h7-8,11H,4-6,9-10H2,1-3H3,(H,18,20);1H/t11-;/m0./s1
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11607043 | https://www.ncbi.nlm.nih.gov/pubmed/1981869
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11607043 | https://www.ncbi.nlm.nih.gov/pubmed/1981869
Remoxipride is a substituted benzamide. It is a weak, but relatively selective, central dopamine D2-receptor antagonist and appears to have preferential affinity for extrastriatal dopamine D2-receptors. It also has marked affinity for central sigma receptors. It was introduced by Astra (Roxiam) at the end of the eighties and was prescribed as an atypical antipsychotic. Remoxipride was withdrawn from the market worldwide by Astra because of several cases of aplastic anaemia associated with the drug.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 2.8 µM [IC50] | |||
Target ID: CHEMBL287 |
60.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ROXIAM Approved UseRemoxipride is primarily indicated in conditions like Schizophrenia, and can also be given in adjunctive therapy as an alternative drug of choice in Psychosis. |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The tolerability and efficacy of the atypical neuroleptic remoxipride compared with clozapine and haloperidol in acute schizophrenia. | 1994 |
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| Remoxipride in Parkinson's disease: differential response in patients with dyskinesias fluctuations versus psychosis. | 1995 Feb |
|
| Differential effects of classical and newer antipsychotics on the hypermotility induced by two dose levels of D-amphetamine. | 1995 Sep 5 |
|
| Remoxipride in the treatment of levodopa-induced psychosis. | 1996 Oct |
|
| Induction of apoptosis by remoxipride metabolites in HL60 and CD34+/CD19- human bone marrow progenitor cells: potential relevance to remoxipride-induced aplastic anemia. | 1999 Aug 1 |
|
| Abused inhalants and central reward pathways: electrophysiological and behavioral studies in the rat. | 2002 Jun |
|
| Chlorpromazine inhibits the glucocorticoid receptor-mediated gene transcription in a calcium-dependent manner. | 2002 Nov |
|
| Differential regulation of hippocampal BDNF mRNA by typical and atypical antipsychotic administration. | 2002 Nov 1 |
|
| Regulation of depotentiation and long-term potentiation in the dentate gyrus of freely moving rats by dopamine D2-like receptors. | 2003 Feb |
|
| Staurosporine-induced apoptosis and hydrogen peroxide-induced necrosis in two human breast cell lines. | 2003 Jan 13 |
|
| New generation antipsychotics versus low-potency conventional antipsychotics: a systematic review and meta-analysis. | 2003 May 10 |
|
| Studies on the effect of MDMA ('ecstasy') on the body temperature of rats housed at different ambient room temperatures. | 2005 Sep |
|
| A dopaminergic deficit hypothesis of schizophrenia: the path to discovery. | 2006 |
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| Inhibitory effect of antipsychotic drugs on the Con A- and LPS-induced proliferative activity of mouse splenocytes: a possible mechanism of action. | 2006 Jun |
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| Sigma 1 receptor-mediated increase in hippocampal extracellular dopamine contributes to the mechanism of the anticonvulsant action of neuropeptide Y. | 2007 Dec |
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| NMDA-mediated release of glutamate and GABA in the subthalamic nucleus is mediated by dopamine: an in vivo microdialysis study in rats. | 2007 Nov |
|
| FemtoMolar measurements using accelerator mass spectrometry. | 2009 Mar |
|
| Zotepine versus other atypical antipsychotics for schizophrenia. | 2010 Oct 6 |
Patents
Sample Use Guides
Two hundred and forty-two patients with acute schizophrenia were enrolled in a double-blind, comparative, dose-finding study of a novel antipsychotic, remoxipride. Remoxipride was evaluated in a low (30 to 90 mg), medium (120 to 240 mg) and a high (300 to 600 mg) dose range and compared with a haloperidol (15 to 45 mg), which was administered to a similar group of patients. The results support the antipsychotic effect of remoxipride, with maximum efficacy occurring at daily doses between 120 mg and 600 mg.
A controlled release (CR) formulation of remoxipride (Roxiam(®), Astra) given once-daily was compared to immediate release (IR) remoxipride given twice-daily, with respect to efficacy and tolerability, in a 4-week multicentre parallel-group dose titration (200-600 mg/day) study with acutely ill schizophrenic patients. Forty- three patients received remoxipride CR (mean dose 344 mg/day) and 49 patients received remoxipride IR (mean dose 346 mg/day).
Route of Administration:
Oral
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m9522
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73220-03-8
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15565709
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ACTIVE MOIETY
SUBSTANCE RECORD
