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Can I read Investigation of Beckett–Casy model 3: Synthesis of novel naltrexone derivatives with contracted and expanded D-rings and their pharmacology on EtoBox?
Investigation of Beckett–Casy model 3: Synthesis of novel naltrexone derivatives with contracted and expanded D-rings and their pharmacology by Hiroshi Nagase; Satomi Imaide; Miyuki Tomatsu; Shigeto Hirayama; Toru Nemoto; Noriko Sato; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Hiroaki Gouda; Shuichi Hirono; Hideaki Fujii is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Investigation of Beckett–Casy model 3: Synthesis of novel naltrexone derivatives with contracted and expanded D-rings and their pharmacology about?
Novel naltrexone derivatives 7 and 8 with contracted and expanded D-rings were synthesized to investigate the importance of orientation of lone electron pair on the nitrogen for binding abilities to the opioid receptor. Compound 7 showed almost no binding affinity, whereas compound 8 was comparable to naltrexone (6) in binding affinity. Conformational analyses and NOE experiments in D(2)O of compounds 6-8 suggested that the lone electron pairs of compounds 6 and 8 with respective six- and seven-membered D-rings would project in the pseudo-axial orientation, whereas compound 7 with five-membered D-ring would have the lone electron pair directing in pseudo-equatorial position. These results strongly supported the proposal that the axial orientation of the lone electron pair on nitrogen would provide sufficient binding abilities to the opioid receptor and that the 15-16 ethylene moiety in the morphine structure would play a role in fixation of the lone electron pair in the axial direction rather than interaction with the putative cavity in the Beckett-Casy model.
Who reads Investigation of Beckett–Casy model 3: Synthesis of novel naltrexone derivatives with contracted and expanded D-rings and their pharmacology?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Hiroshi Nagase; Satomi Imaide; Miyuki Tomatsu; Shigeto Hirayama; Toru Nemoto; Noriko Sato; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Hiroaki Gouda; Shuichi Hirono; Hideaki Fujii
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2010
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)