کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9921486 | 1559224 | 2005 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism
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موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism](/preview/png/9921486.png)
چکیده انگلیسی
In the search for opioid agonists with delayed antagonist actions as potential treatments for substance abuse, the bridged morphinan BU74 (17-cyclopropylmethyl-3-hydroxy-[5β,7β,3â²,5â²]-pyrrolidino-2â²[S]-phenyl-7α-methyl-6,14-endoetheno morphinan) (3f) was synthesized. In isolated tissue and [35S]GTPγS opioid receptor functional assays BU74 was shown to be a potent long-lasting kappa opioid receptor agonist, delta opioid receptor partial agonist and mu opioid receptor antagonist. In antinociceptive tests in the mouse, BU74 showed high efficacy and potent kappa opioid receptor agonism. When its agonist action had waned BU74 became an antagonist of kappa and mu opioid receptor agonists in the tail flick assay and of delta, kappa and mu opioid receptor agonists in the acetic acid writhing assay. The slow onset, long-duration kappa opioid receptor agonist effects of BU74 suggests that it could be a lead compound for the discovery of a treatment for cocaine abuse.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 509, Issues 2â3, 21 February 2005, Pages 117-125
Journal: European Journal of Pharmacology - Volume 509, Issues 2â3, 21 February 2005, Pages 117-125
نویسندگان
Stephen M. Husbands, Claire L. Neilan, Jillian Broadbear, Peter Grundt, Simon Breeden, Mario D. Aceto, James H. Woods, John W. Lewis, John R. Traynor,