کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5824309 | 1118486 | 2007 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Molecular cloning, mutations and effects of NK1 receptor antagonists reveal the human-like pharmacology of gerbil NK1 receptors
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کلمات کلیدی
MRMNKANK1RGFTLC–MS - LC-MSisoleucine - ایولولینIle - باCho - برایChinese Hamster Ovary - تخمدان هامستر چینیSite directed mutagenesis - سایت موتاگنسیس را هدایت می کندliquid chromatography–mass spectrometry - طیف سنجی جرم کروماتوگرافی مایعSubstance P - ماده PHomology models - مدل های همگراmultiple reaction monitoring - نظارت چندگانه چندگانهneurokinin - نورو کینینneurokinin A - نورو کینین Ahigh performance liquid chromatography - کروماتوگرافی مایع با کارایی بالاHPLC - کروماتوگرافی مایعی کاراGerbil - گربیلNeurokinin 1 receptor - گیرنده neurokinin 1
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
داروشناسی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Molecular cloning, mutations and effects of NK1 receptor antagonists reveal the human-like pharmacology of gerbil NK1 receptors Molecular cloning, mutations and effects of NK1 receptor antagonists reveal the human-like pharmacology of gerbil NK1 receptors](/preview/png/5824309.png)
چکیده انگلیسی
The gNK1R coding sequence displayed an overall 95% and 97% homology with hNK1R and rNK1R, respectively. The affinity of the NK1R-selective agonist 3H-SarMet SP for human and gerbil NK1R was similar (2.0 and 3.1 nM) but lower for rNK1R (12.4 nM). The rank order potency of the agonists for NK1R was SP â¥Â ASMSP â¥Â NKA â pro7NKB in all species. The NK1R antagonists, ZD6021 and CP99994, had comparable affinity and potency for gerbil and human NK1R, but were 1000-fold less potent for rNK1R. In contrast, RP67580 had comparable affinity and potency for all three species. Mutations in positions 116 and 290 did not affect agonist potency at the gNK1R while the potency of the antagonists ZD6021 and CP99994 were markedly decreased (10-20-fold). It is concluded that gNK1R has similar antagonist pharmacology as the human-like orthologue and that species differences in antagonist function depend on key residues in the coding sequence and antagonist structure.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 73, Issue 2, 15 January 2007, Pages 259-269
Journal: Biochemical Pharmacology - Volume 73, Issue 2, 15 January 2007, Pages 259-269
نویسندگان
Susanna Engberg, Ingela Ahlstedt, Agnes Leffler, Erik Lindström, Elin Kristensson, Arne Svensson, Ingrid PÃ¥hlman, Anders Johansson, Tomas Drmota, Bengt von Mentzer,