A-834,735

http://dbpedia.org/resource/A-834,735 an entity of type: Thing

A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a Ki of 12 nM at CB1 and 0.21 nM at CB2. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids, with the 3-tetramethylcyclopropylmethanone group of A-834,735 and related compounds, imparts significant selectivity for CB2, with most compounds from this group found to be highly selective CB2 agonists with little affinity for CB1. However low nanomolar CB1 binding affinity is retained with certain heterocyclic 1-position substituents such as (N-methylpiperidin-2-yl)methyl (cf. AM-1220, AM-1248), or the (tetrahydropyran-4-yl)methyl substituent of A-834,735, resulting in compounds that still show significan rdf:langString
rdf:langString A-834,735
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xsd:integer 1082421017
xsd:integer 22
xsd:integer 895155
xsd:integer 271158
xsd:integer 9719418
xsd:integer 29
rdf:langString {1-[methyl]-1H-indol-3-yl}-methanone
rdf:langString Class B
xsd:integer 1
xsd:integer 2
xsd:integer 11544639
rdf:langString C4COCCC4Cnc2ccccc2c3CC1CC1C
xsd:integer 1
rdf:langString NQTMRZNYLIGQCF-UHFFFAOYSA-N
rdf:langString XE27L67C93
rdf:langString changed
xsd:integer 456505675
rdf:langString changed
rdf:langString A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a Ki of 12 nM at CB1 and 0.21 nM at CB2. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids, with the 3-tetramethylcyclopropylmethanone group of A-834,735 and related compounds, imparts significant selectivity for CB2, with most compounds from this group found to be highly selective CB2 agonists with little affinity for CB1. However low nanomolar CB1 binding affinity is retained with certain heterocyclic 1-position substituents such as (N-methylpiperidin-2-yl)methyl (cf. AM-1220, AM-1248), or the (tetrahydropyran-4-yl)methyl substituent of A-834,735, resulting in compounds that still show significant affinity and efficacy at both receptors despite being CB2 selective overall.
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xsd:string 895155-57-4
xsd:string 271158
xsd:string XE27L67C93
xsd:string 11544639

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