Brasofensine
http://dbpedia.org/resource/Brasofensine an entity of type: Thing
Brasofensine (NS-2214, BMS-204756) is a phenyltropane that had been under development by Bristol-Myers Squibb for the treatment of Parkinson's and Alzheimer's diseases. In animal models of Parkinson's disease, brasofensine was effective in stimulating LMA and reversing akinesia. Phase II trials in humans were conducted in 1996 and brasofensine was shown to be both effective and well tolerated at a dose of 4 mg; however, development was stopped after in vivo cis-anti isomerization of the 2α-methyloxime group was reported.
rdf:langString
rdf:langString
Brasofensine
xsd:integer
12862491
xsd:integer
1084614430
rdf:langString
none
xsd:integer
16
xsd:integer
171655
xsd:integer
2104184
xsd:integer
7888898
xsd:integer
2
xsd:integer
20
rdf:langString
--1-[-3--8-methyl-8-azabicyclo[3.2.1]octane-2-carbaldehyde O-methyloxime
rdf:langString
Class A
xsd:integer
2
xsd:integer
1
xsd:integer
9614919
rdf:langString
Clc1ccc[C@H]3C[C@H]2N[C@H][C@@H]3\C=N\OC
xsd:integer
1
rdf:langString
NRLIFEGHTNUYFL-QJDHNRDASA-N
xsd:integer
1
rdf:langString
changed
xsd:integer
437723330
rdf:langString
Brasofensine (NS-2214, BMS-204756) is a phenyltropane that had been under development by Bristol-Myers Squibb for the treatment of Parkinson's and Alzheimer's diseases. In animal models of Parkinson's disease, brasofensine was effective in stimulating LMA and reversing akinesia. Phase II trials in humans were conducted in 1996 and brasofensine was shown to be both effective and well tolerated at a dose of 4 mg; however, development was stopped after in vivo cis-anti isomerization of the 2α-methyloxime group was reported. The isomerization of brasofensine did not involve epimerization at 2-position of the tropane ring, but rather involved the E/Z-isomerization of the imine (i.e. "methyl-aldoxime"). It was believed that this process occurs in vivo, although it cannot be ruled out as a possibility that some isomerization also occurs prior to ingestion. The (Z)-isomer has been assigned the name BMS-205912. In Parkison's disease, symptoms do not begin to manifest until there has been an 80% reduction in dopaminergic neurons, particularly in the substantia nigra brain region.
xsd:nonNegativeInteger
5330
xsd:string
171655-91-7
xsd:string
2104184
xsd:string
1YP2S94RVH
xsd:string
9614919