کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
8993437 1113800 2005 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Rigid analogs of DMPP as probes for the nicotinic receptors
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Rigid analogs of DMPP as probes for the nicotinic receptors
چکیده انگلیسی
Chemical manipulation of the nicotinic agonist DMPP, endowed with modest activity on the central receptors, definitely improved its affinity and pharmacokinetic properties. Although their pharmacophore is somehow different from that of classical nicotinic ligands, some DMPP derivatives show low nanomolar affinity for the central nicotinic receptors. Introduction of rigidity in the structure of DMPP and in that of its analogue 1-(3-pyridyl)piperazine, resulted in molecules with lower or null affinity for the central nicotinic receptors. This suggests that the frozen structures chosen either do not represent the bioactive conformation, or their volume is not compatible with the space available within the interaction site.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Il Farmaco - Volume 60, Issue 2, February 2005, Pages 99-104
نویسندگان
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