دورية أكاديمية
Biological effects on μ-receptors affinity and selectivity of aryl propenyl chain structural modification on diazatricyclodecane derivatives
| العنوان: | Biological effects on μ-receptors affinity and selectivity of aryl propenyl chain structural modification on diazatricyclodecane derivatives |
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| المؤلفون: | Piras S., Murineddu G., Loriga G., Carta A., Battistello E., Merighi S., Gessi S., Corona P., Asproni B., Ibba R., Temml V., Schuster D., Pinna G. A. |
| المساهمون: | Piras, S., Murineddu, G., Loriga, G., Carta, A., Battistello, E., Merighi, S., Gessi, S., Corona, P., Asproni, B., Ibba, R., Temml, V., Schuster, D., Pinna, G. A. |
| سنة النشر: | 2021 |
| المجموعة: | Università degli Studi di Ferrara: CINECA IRIS |
| مصطلحات موضوعية: | μ-receptors affinity, analgesic activity, 9,10-diazatricyclo[4.2.1.12,5]decane (DTD), 2,7- diazatricyclo[4.4.0.03,8]decane, DTD derivatives, rigid benzo-condensed structure |
| الوصف: | Opioid analgesics are clinically used to relieve severe pain in acute postoperative and cancer pain, and also in the long term in chronic pain. The analgesic action is mediated by μ-, δ-, and κ-receptors, but currently, with few exceptions for k-agonists, μ-agonists are the only ones used in therapy. Previously synthesized compounds with diazotricyclodecane cores (DTDs) have shown their effectiveness in binding opioid receptors. Fourteen novel diazatricyclodecanes belonging to the 9-propionyl-10-substituted-9,10-diazatricyclo[4.2.1.12,5]decane (compounds 20–23, 53, 57 and 59) and 2-propionyl-7-substituted-2,7-diazatricyclo[4.4.0.03,8]decane (compounds 24–27, 54, 58 and 60) series, respectively, have been synthesized and their ability to bind to the opioid μ-, δ-and κ-receptors was evaluated. Five of these derivatives, compounds 20, 21, 24, 26 and 53, showed μ-affinity in the nanomolar range with a negligible affinity towards δ-and κ-receptors and high μ-receptor selectivity. The synthesized compounds showed μ-receptor selectivity higher than those of previously reported methylarylcinnamyl analogs. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | STAMPA |
| اللغة: | English |
| العلاقة: | info:eu-repo/semantics/altIdentifier/pmid/34576918; info:eu-repo/semantics/altIdentifier/wos/WOS:000701272600001; volume:26; issue:18; firstpage:5448-1; lastpage:5448-19; numberofpages:19; journal:MOLECULES; https://hdl.handle.net/11392/2474890Test; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85114612247; https://www.mdpi.com/1420-3049/26/18/5448Test |
| DOI: | 10.3390/molecules26185448 |
| الإتاحة: | https://doi.org/10.3390/molecules26185448Test https://hdl.handle.net/11392/2474890Test https://www.mdpi.com/1420-3049/26/18/5448Test |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.C40FF68F |
| قاعدة البيانات: | BASE |
| DOI: | 10.3390/molecules26185448 |
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