In Vitro selectivity of an acyclic cucurbit[n]uril molecular container towards neuromuscular blocking agents relative to commonly used drugs
Author:
Affiliation:
1. Department of Chemistry and Biochemistry
2. University of Maryland
3. College Park
4. USA
5. Department of Anesthesia
6. Critical Care and Pain Medicine
7. Massachusetts General Hospital
8. and Harvard Medical School
9. Boston
Abstract
We measure the binding affinity of Calabadion 2 toward 27 drugs to assess its selectivity toward rocuronium, vecuronium, and cisatracurium.
Funder
Massachusetts General Hospital
National Cancer Institute
Publisher
Royal Society of Chemistry (RSC)
Subject
Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2016/OB/C5OB02356D
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4. Cyclodextrin-Derived Host Molecules as Reversal Agents for the Neuromuscular Blocker Rocuronium Bromide: Synthesis and Structure−Activity Relationships
5. A Novel Concept of Reversing Neuromuscular Block: Chemical Encapsulation of Rocuronium Bromide by a Cyclodextrin-Based Synthetic Host The discovery of Org 25969 is the result of teamwork with contributions from a number of scientists both inside Organon and outside the company. We would like in particular to acknowledge the following scientists for their invaluable contributions: E. Hutchinson, D. Stevenson, R. Roy, and J. Pick for scaling-up the synthesis; F. Hope, S. Miller, and R. Mason for various in vitro and in vivo pharmacological testing; R. Watson, B. Montgomery, P. Desmond, and A. Osprey for all their analytical effort; and R. McGuire and J. Mestres for graphical presentation of the X-ray crystal structure of the Org 25969–rocuronium complex (Figure 3). We would also like to thank Prof. A. Cooper of Glasgow University who has critically reproduced our calorimetry data of Org 25969–rocuronium complexation (Figure 2).
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