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

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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