Synthesis and Pharmacological Evaluation of Novel 9- and 10-Substituted Cytisine Derivatives. Nicotinic Ligands of Enhanced Subtype Selectivity
Sheela K. ChellappanDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, Department of Pharmacology, Georgetown University, 3900 Reservoir Road, NW, Washington, D.C. 20057, and Acenta Discovery Inc, 9030 S. Rita Road, Suite 300, Tucson, Arizona 85747Yingxian XiaoDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, Department of Pharmacology, Georgetown University, 3900 Reservoir Road, NW, Washington, D.C. 20057, and Acenta Discovery Inc, 9030 S. Rita Road, Suite 300, Tucson, Arizona 85747W. TUECKMANTELDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, Department of Pharmacology, Georgetown University, 3900 Reservoir Road, NW, Washington, D.C. 20057, and Acenta Discovery Inc, 9030 S. Rita Road, Suite 300, Tucson, Arizona 85747Kenneth J. KellarDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, Department of Pharmacology, Georgetown University, 3900 Reservoir Road, NW, Washington, D.C. 20057, and Acenta Discovery Inc, 9030 S. Rita Road, Suite 300, Tucson, Arizona 85747Alan P. KozikowskiDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, Department of Pharmacology, Georgetown University, 3900 Reservoir Road, NW, Washington, D.C. 20057, and Acenta Discovery Inc, 9030 S. Rita Road, Suite 300, Tucson, Arizona 85747
2006en
ABI
Annotatsiya
We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the alpha4beta2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.
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