Title of article
A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay Original Research Article
Author/Authors
Emilie D. Smith، نويسنده , , N. Ariane Vinson، نويسنده , , Desong Zhong، نويسنده , , Bertold D. Berrang، نويسنده , , Jennifer L. Catanzaro، نويسنده , , James B. Thomas، نويسنده , , Hern?n A. Navarro، نويسنده , , Brian P. Gilmour، نويسنده , , Jeffrey Deschamps، نويسنده , , F. Ivy Carroll، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
8
From page
822
To page
829
Abstract
A new chiral synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (2, J-113397) was developed. J-113397 has a Ke = 0.85 nM in an ORL-1 calcium mobilization assay and is 89-, 887-, and 227-fold selective for the ORL-1 receptor relative to the μ, δ, and κ opioid receptors.
Keywords
Protein tyrosine kinase inhibitors , QSAR analysis , 2D Autocorrelation space , CoMFA , CoMSIA
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1303952
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