Brasofensine is an orally administered dopamine reuptake inhibitor being developed for the treatment of Parkinson's Disease. Phase I/II trials for brasofensine have been completed in the U.K. In November 2001, NeuroSearch confirmed that the drug's development was discontinued in favor of NS 2230.
|External IDs||BMS-204756 / NS-2214|
|Product Ingredients||Not Available|
|Approved Prescription Products||Not Available|
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|Weight||Average: 327.25 |
For the treatment of Parkinson's Disease.
|Structured Indications||Not Available|
Brasofensine is an inhibitor of the synaptic dopamine transporter. It is a geometric isomer of the E-form; the Z-isomer is denoted as BMS-205912.
|Mechanism of action|
When the neurotransmitter dopamine is released into the synaptic cleft, brasofensine prevents it from entering back into the source nerve cell, thereby allowing a longer period of synaptic activity.
Brasofensine is rapidly absorbed after oral administration in rats and monkeys, with peak plasma concentrations occurring 0.5-1 hr, but 3-8 hr for brasofensine in humans.
|Volume of distribution||Not Available|
|Protein binding||Not Available|
Brasofensine undergoes extensive first-pass metabolism following oral administration in humans, monkeys, and rats. It primarily underwent O- and N-demethylation and isomerization. Some of the desmethyl metabolites were further converted to glucuronides. These primary metabolites and glucuronides of demethyl brasofensine (M1 and M2) were major circulating metabolites in humans, and were also observed in rat and monkey plasma.
|Route of elimination||Not Available|
Plasma terminal elimination half-lives were ~2 hr in rats, ~4 hr in monkeys, but ~24 hr in humans.
|Pharmacogenomic Effects/ADRs||Not Available|
|Drug Interactions||Not Available|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
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|Experimental Properties||Not Available|
|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of organic compounds known as phenyltropanes. These are compounds containing a phenyl group linked to a tropane moiety. Tropane is an organonitrogenous [3.2.1] bicyclic organic compound.|
|Super Class||Alkaloids and derivatives|
|Alternative Parents||Phenylpiperidines / Dichlorobenzenes / Aralkylamines / N-alkylpyrrolidines / Aryl chlorides / Trialkylamines / Oxime ethers / Azacyclic compounds / Organooxygen compounds / Organochlorides / Hydrocarbon derivatives|
|Substituents||Phenyltropane / Phenylpiperidine / 1,2-dichlorobenzene / Aralkylamine / Chlorobenzene / Halobenzene / Aryl chloride / Aryl halide / Benzenoid / N-alkylpyrrolidine/ Monocyclic benzene moiety / Piperidine / Pyrrolidine / Tertiary aliphatic amine / Tertiary amine / Oxime ether / Organoheterocyclic compound / Azacycle / Organonitrogen compound / Organochloride / Organohalogen compound / Organic oxygen compound / Amine / Hydrocarbon derivative / Organooxygen compound / Organic nitrogen compound / Aromatic heteropolycyclic compound|
|Molecular Framework||Aromatic heteropolycyclic compounds|
|External Descriptors||Not Available|
- Pharmacological action
- General Function:
- Potassium channel regulator activity
- Specific Function:
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- D(2) dopamine receptor
- Molecular Weight:
- 50618.91 Da
- Zhu M, Whigan DB, Chang SY, Dockens RC: Disposition and metabolism of [14C]brasofensine in rats, monkeys, and humans. Drug Metab Dispos. 2008 Jan;36(1):24-35. Epub 2007 Oct 1. [PubMed:17908924 ]