کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2008634 | 1066434 | 2006 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Partial and full agonism in endomorphin derivatives: Comparison by null and operational model
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موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
The partial μ-opioid receptor pool inactivation strategy in isolated mouse vas deferens was used to determine partial agonism of endomorphins and their analogs (endomorphin-1-ol, 2â²,6â²-dimethyltyrosine (Dmt)-endomorphin-1, endomorphin-2-ol and (d-Met2)-endomorphin-2) using morphine, normorphine, morphiceptin, (d-Ala2,MePhe4,Gly5-ol)-enkephalin (DAMGO) and its amide (DAMGA) as reference opioid agonists. Agonist affinities (KA) and efficacies were assessed both by the “null” and the “operational” method. The KA values determined by the two methods correlated significantly with each other and also with the displacing potencies against 3H-naloxone in the receptor binding assay in the presence of Na+. DAMGO and DAMGA were full agonist prototypes, morphine, endomorphin-1, endomorphin-1-ol, Dmt-endomorphin-1, endomorphin-2-ol and (d-Met2)-endomorphin-2 were found by both methods to be partial agonists whereas the parameters for normorphine, morphiceptin and endomorphin-2 were intermediate.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Peptides - Volume 27, Issue 6, June 2006, Pages 1507-1513
Journal: Peptides - Volume 27, Issue 6, June 2006, Pages 1507-1513
نویسندگان
András Z. Rónai, Mahmoud Al-Khrasani, Sándor Benyhe, Imre Lengyel, László Kocsis, György Orosz, Géza Tóth, Erzsébet Kató, László Tóthfalusi,