Design and Synthesis of m1-Selective Muscarinic Agonists:  (R)-(−)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3‘-Methoxyphenyl)-2-propynyl)- oxime Maleate (CI-1017), a Functionally m1-Selective Muscarinic Agonist

Autor: Tecle, H., Barrett, S. D., Lauffer, D. J., Augelli-Szafran, C., Brann, M. R., Callahan, M. J., Caprathe, B. W., Davis, R. E., Doyle, P. D., Eubanks, D., Lipiniski, W., Mirzadegan, T., Moos, W. H., Moreland, D. W., Nelson, C. B., Pavia, M. R., Raby, C., Schwarz, R. D., Spencer, C. J., Thomas, A. J., Jaen, J. C.
Zdroj: Journal of Medicinal Chemistry; July 2, 1998, Vol. 41 Issue: 14 p2524-2536, 13p
Abstrakt: The synthesis and SAR of a series of (Z)-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl)oximes are described. The biochemistry and pharmacology of 24Z (PD 142505) and its enantiomers are highlighted. 24Z is functionally an m1-selective muscarinic agonist. Efficacy and m1 selectivity reside in the R enantiomer, (R)-24Z (CI-1017).
Databáze: Supplemental Index