Title of article
The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptor
Author/Authors
Nicholas J. Murgolo، نويسنده , , Joseph Kozlowski، نويسنده , , Melissa A. B. Tice، نويسنده , , Frank P. Hollinger، نويسنده , , Joan E. Brown، نويسنده , , Guowei Zhou، نويسنده , , Lisa A. Taylor، نويسنده , , Robert D. McQuade، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1996
Pages
4
From page
785
To page
788
Abstract
An analog (SCH55112) of pirenzepine was prepared in which the N4 piperazyl nitrogen was replaced with carbon. This structrual change abolished the 55-fold m1/m2 selectivity of pirenzepine due to specific loss of m1 affinity. Mutagenesis mapping and modeling studies suggested this change was due to loss of a hydrogen bond to m1 Thr32 (m2Ala30).
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1996
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
788000
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