Abstract：
:Anandamide (arachidonylethanolamide), isolated from porcine brain, has been shown to bind to the cannabinoid receptor and also to produce cannabimimetic activity in pharmacological assays. This study examined structure-activity relationships in alkylated anandamide analogs. The analogs were evaluated for their ability to displace [3H]CP-55,940 in a filtration binding assay using rat brain membranes in the presence and absence of the enzyme inhibitor phenylmethylsulfonyl fluoride (PMSF). Behavioral activity was assessed by the ability of the analogs to produce hypomotility and antinociception. Methylations at carbons 2 and 1 produced compounds stable in the absence of PMSF with similar affinities and behavioral activity as anandamide. Addition of larger alkyl groups at these positions or nitrogen methylation reduced receptor affinity and behavioral potency. These results indicate that methylations at specific carbons of anandamide confer stability in vitro.
journal_name
Life Scijournal_title
Life sciencesauthors
Adams IB,Ryan W,Singer M,Razdan RK,Compton DR,Martin BRdoi
10.1016/0024-3205(95)00187-bsubject
Has Abstractpub_date
1995-01-01 00:00:00pages
2041-8issue
23-24eissn
0024-3205issn
1879-0631pii
0024-3205(95)00187-Bjournal_volume
56pub_type
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