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

Haile Tecle; Stephen D. Barrett; David Lauffer; Corinne E. Augelli‐Szafran; Mark R. Brann; Michael J. Callahan; Bradley W. Caprathe; Robert E. Davis; Patricia D. Doyle; David C. Eubanks; William Lipiniski; Tara Mirzadegan; Walter H. Moos; D.W. Moreland; Carrie B. Nelson; Michael R. Pavia; C Raby; Roy D. Schwarz; Carolyn J. Spencer; Anthony J. Thomas; Juan C. Jaén

doi:10.1021/jm960683m

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Abstract

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).

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Tecle et al. (1998) studied this question.

synapsesocial.com/papers/6a830ae9e1ce079453581f07 https://doi.org/10.1021/jm960683m

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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

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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

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