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Please use this identifier to cite or link to this item:
http://hdl.handle.net/123456789/17131
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| Title: | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| Authors: | Stefan LÃber
Tarek Aboul-Fadl
Peter Gmeiner |
| Keywords: | Dopamine Agonists, Humans, Ligands, Protein Binding, Pyrazoles, Pyridines, Receptors, Dopamine, Receptors, Dopamine D2, Receptors, Dopamine D4, Structure-Activity Relationship, metabolism, pharmacology, chemistry |
| Issue Date: | 2002 |
| Publisher: | BIOORGANIC |
| Abstract: | Based on the lead molecule FAUC 113, a series of di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives was synthesized and investigated for their dopamine receptor binding profile. The carbonitrile 11a (FAUC 327) showed excellent pharmacological properties combining high D4 affinity (K(i)=1.5 nM) and selectivity with significant intrinsic activity (31%) in low nanomolar concentrations (EC50=1.5 nM). |
| URI: | http://hdl.handle.net/123456789/17131 |
| Appears in Collections: | College of Pharmacy
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