کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374396 | 981918 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype](/preview/png/1374396.png)
چکیده انگلیسی
Aminomethyl-substituted biaryls bearing a pyrazole or triazole moiety were synthesized and investigated for dopamine and serotonin receptor binding. The N-arylpyrazoles 3b,f,g and 4 revealed Ki values in the subnanomolar range (0.28–0.70 nM) for the dopamine D4 receptor subtype. Employing both mitogenesis and GTPγS assays, ligand efficacy was evaluated indicating partial agonist properties. Interestingly, the tetrahydropyrimidine 4 (FAUC 2020) displayed significant intrinsic selectivity for D2long over D2short.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 11, 1 June 2006, Pages 2955–2959
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 11, 1 June 2006, Pages 2955–2959
نویسندگان
Stefan Löber, Harald Hübner, Peter Gmeiner,