Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.
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Cha JH, Cho YS, Pae AN, Koh HY, Jeong D, Kong JY, Lee E, Choi KI
Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.
Bioorg Med Chem Lett. 2001 Nov 5;11(21):2855-7.
- PubMed ID
- 11597415 [ View in PubMed]
- Abstract
Two series of compounds, 2 and 3, were synthesized and their binding affinities were evaluated for the human recombinant muscarinic M(1) receptor subtype expressed in CHO cells. Comparing their binding affinities for the NMS binding sites and the Oxo-M binding sites, they were assumed as agonists. In particular, compound 2e was a good ligand for the agonist binding sites with an IC(50) of 23 nM, which represents over 1585 times stronger binding than for the antagonist binding sites.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Arecoline Muscarinic acetylcholine receptor M1 IC 50 (nM) 115 N/A N/A Details Arecoline Muscarinic acetylcholine receptor M1 IC 50 (nM) 115500 N/A N/A Details