Journal
CHEMBIOCHEM
Volume 18, Issue 16, Pages 1583-1588Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201700289
Keywords
calabadion; drugs of abuse; methamphetamine; molecular container; reversal agent
Funding
- National Institutes of Health [CA168365]
- University of Maryland
- Merck Inc.
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We measured the affinity of five molecular container compounds (calabadions 1 and 2, CB[7], sulfocalix[4]arene, and HP--CD) toward seven drugs of abuse in homogenous aqueous solution at physiological pH by various methods ((HNMR)-H-1, UV/Vis, isothermal titration calorimetry [ITC]) and found binding constants (K-a values) spanning from <10(2) to >10(8)m(-1). We also report X-ray crystal structures of CB[7]methamphetamine and 1methamphetamine. We found that 2, but not CB[7], was able to ameliorate the hyperlocomotive activity of rats treated with methamphetamine. The bioavailability of the calabadions and their convergent building block synthesis suggest potential for further structural optimization as reversal agents for intoxication with nonopioid drugs of abuse for which no treatments are currently available.
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